- Convergent synthesis of dronedarone, an antiarrhythmic agent
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We have developed a convergent synthesis of dronedarone, an antiarrhythmic agent. The key steps of the process are the construction of a benzofuran skeleton by iodocyclization and the carbonylative Suzuki-Miyaura cross-coupling for biaryl ketone formation. This synthetic route required only eight steps from 2-amino-4-nitrophenol in 23% overall yield.
- Okitsu, Takashi,Ogasahara, Mizuki,Wada, Akimori
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- Concise total synthesis of antiarrhythmic drug dronedarone via a conjugate addition followed intramolecular heck cyclization
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A concise, scalable, and an efficient total synthesis for dronedarone (2) was described using conjugate addition followed by intramolecular Heck cyclization. The other key reaction includes selective reduction of nitro functionality and addition of lithiated terminal alkyne to the aldehyde. The overall yield of this approach is 44% in six steps.
- Madhasu, Madhu,Doda, Sai Reddy,Begari, Prem Kumar,Dasari, Krishna Rao,Thalari, Gangadhar,Kadari, Sudhakar,Yadav, Jhillu Singh
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p. 1861 - 1866
(2021/07/09)
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- Visible-Light-Induced Radical Carbo-Cyclization/ gem-Diborylation through Triplet Energy Transfer between a Gold Catalyst and Aryl Iodides
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Geminal diboronates have attracted significant attention because of their unique structures and reactivity. However, benzofuran-, indole-, and benzothiophene-based benzylic gem-diboronates, building blocks for biologically relevant compounds, are unknown. A promising protocol using visible light and aryl iodides for constructing valuable building blocks, including benzofuran-, indole-, and benzothiophene-based benzylic gem-diboronates, via radical carbo-cyclization/gem-diborylation of alkynes with a high functional group tolerance is presented. The utility of these gem-diboronates has been demonstrated by a 10 g scale conversion, by versatile transformations, by including the synthesis of approved drug scaffolds and two approved drugs, and even by polymer synthesis. The mechanistic investigation indicates that the merging of the dinuclear gold catalyst (photoexcitation by 315-400 nm UVA light) with Na2CO3 is directly responsible for photosensitization of aryl iodides (photoexcitation by 254 nm UV light) with blue LED light (410-490 nm, λmax = 465 nm) through an energy transfer (EnT) process, followed by homolytic cleavage of the C-I bond in the aryl iodide substrates.
- Hashmi, A. Stephen K.,Rominger, Frank,Si, Xiaojia,Zhang, Lumin
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p. 10485 - 10493
(2020/07/03)
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- Efficient Syntheses of Diverse, Medicinally Relevant Targets Planned by Computer and Executed in the Laboratory
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The Chematica program was used to autonomously design synthetic pathways to eight structurally diverse targets, including seven commercially valuable bioactive substances and one natural product. All of these computer-planned routes were successfully executed in the laboratory and offer significant yield improvements and cost savings over previous approaches, provide alternatives to patented routes, or produce targets that were not synthesized previously. Although computers have demonstrated the ability to challenge humans in various games of strategy, their use in the automated planning of organic syntheses remains unprecedented. As a result of the impact that such a tool could have on the synthetic community, the past half century has seen numerous attempts to create in silico chemical intelligence. However, there has not been a successful demonstration of a synthetic route designed by machine and then executed in the laboratory. Here, we describe an experiment where the software program Chematica designed syntheses leading to eight commercially valuable and/or medicinally relevant targets; in each case tested, Chematica significantly improved on previous approaches or identified efficient routes to targets for which previous synthetic attempts had failed. These results indicate that now and in the future, chemists can finally benefit from having an “in silico colleague” that constantly learns, never forgets, and will never retire. Multistep synthetic routes to eight structurally diverse and medicinally relevant targets were planned autonomously by the Chematica computer program, which combines expert chemical knowledge with network-search and artificial-intelligence algorithms. All of the proposed syntheses were successfully executed in the laboratory and offer substantial yield improvements and cost savings over previous approaches or provide the first documented route to a given target. These results provide the long-awaited validation of a computer program in practically relevant synthetic design.
- Klucznik, Tomasz,Mikulak-Klucznik, Barbara,McCormack, Michael P.,Lima, Heather,Szymku?, Sara,Bhowmick, Manishabrata,Molga, Karol,Zhou, Yubai,Rickershauser, Lindsey,Gajewska, Ewa P.,Toutchkine, Alexei,Dittwald, Piotr,Startek, Micha? P.,Kirkovits, Gregory J.,Roszak, Rafa?,Adamski, Ariel,Sieredzińska, Bianka,Mrksich, Milan,Trice, Sarah L.J.,Grzybowski, Bartosz A.
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p. 522 - 532
(2018/03/21)
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- A short synthesis of Dronedarone
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A modification of the Nenitzescu reaction was used to obtain Dronedarone from quinonimine 20 and 1,3-diketone 14 (R = CH2CH2CH2NBu2) in a two-stage process in almost 55% overall yield. Our results represent significant improvement over other state-of-the-art methods as no extra steps for the decoration of the benzofuran core are required.
- Piotrkowska, Barbara,Nerdinger, Sven,Schreiner, Erwin,Seli?, Lovro,Graczyk, Piotr P.
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p. 4330 - 4335
(2018/05/04)
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- PROCESS FOR PREPARATION OF DRONEDARONE BY REMOVAL OF HYDROXYL GROUP
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The invention relates to a process for preparation of dronedarone of formula (I) and pharmaceutically acceptable salts thereof characterized in that from the compound of formula (II). the hydroxyl group is removed, and the obtained product is isolated and, if desired, converted into a pharmaceutically acceptable salt thereof.
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Paragraph 0075
(2015/02/05)
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- PROCESS FOR THE PREPARATION OF DRONEDARONE BY OXIDATION OF A SULPHENYL GROUP
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The invention relates to a novel process for the preparation of dronedarone (I) and pharmaceutically acceptable salts thereof which comprises oxidizing a compound of formula (IV) or a salt thereof with an oxidizing agent in an organic or inorganic solvent or solvent mixture, and isolating the obtained product and, if desired, converting it into a pharmaceutically acceptable salt thereof. Further aspects of the invention include the novel intermediary compound of formula (IV), and a process for the preparation thereof.
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Paragraph 0065; 0066; 0067
(2015/02/19)
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- A facile and efficient synthesis of dronedarone hydrochloride
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A facile and efficient synthesis of dronedarone hydrochloride starting from commercially available 4- nitrophenol is described. This approach features a tandem-type synthesis of 3-carbonylated benzofuran involving cyclization of 2-ethynylphenol followed by CO2 fixation at the 3-position of the benzofuran ring mediated by potassium carbonate without the addition of any transition metal catalyst.
- Li, Feng,Jin, Chunhua,Zou, Jianwei,Wu, Jun
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p. 1970 - 1972
(2014/09/17)
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- Identification and characterization of potential impurities of dronedarone hydrochloride
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Six potential process related impurities were detected during the impurity profile study of an antiarrhythmic drug substance, Dronedarone (1). Simple high performance liquid chromatography and liquid chromatography-mass spectrometry methods were used for the detection of these process impurities. Based on the synthesis and spectral data (MS, IR, 1H NMR, 13C NMR, and DEPT), the structures of these impurities were characterized a s 5-amino-3-[4-(3-di-n-butylaminopropoxy)benzoyl]-2-n-butylbenzofuran (impurity I); N-(2-butyl-3-(4-(3-(dibutylamino)propoxy)-benzoyl)benzofuran-5-yl)-N- (methylsulfonyl)-methanesulfonamide (impurity II); N-(2-butyl-3-(4-(3- (dibutylamino)propoxy)benzoyl)benzofuran-5-yl)-1-chloromethanesulfonamide (impurity III); N-{2-propyl-3-[4-(3-dibutylaminopropoxy)benzoyl]benzofuran-5-yl} - methanesulfonamide (impurity IV); N-(2-butyl-3-(4-(3-(dibutylamino)propoxy) benzoyl)benzofuran-5-yl)-formamide (impurity V); and (2-butyl-5-((3- (dibutylamino)propyl)amino)benzofuran-3-yl)(4-(3- (dibutylamino)propoxy)phenyl) methanone (impurity VI). The synthesis and characterization of these impurities are discussed in detail.
- Mahender,Saravanan,Sridhar,Chandrashekar,Kumar, L. Jaydeep,Jayashree,Bandichhor, Rakeshwar
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p. 157 - 162
(2014/05/20)
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- PROCESS FOR SYNTHESIZING KETO-BENZOFURAN DERIVATIVES
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The invention relates to a process for synthesizing benzofuran derivatives, in particular dronedarone of formula (D), comprising a step of Friedel-Crafts acylation starting from a sulfonamido-benzofuran ester intermediate.
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- REDUCTIVE AMINATION PROCESS FOR PREPARATION OF DRONEDARONE USING AMINE INTERMEDIARY COMPOUND
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The invention relates to a novel process for preparation of drohedarone of formula (I) and pharmaceutically acceptable salts thereof characterized in that a compound of formula (II) is reacted in the presence of a reductive agent with butyraldehyde and/or butanoic acid, and isolating the obtained product and, if desired, converting it into a pharmaceutically acceptable salt thereof. The invention also relates to some hovel intermediary compounds and the preparation thereof.
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Paragraph 0126-0127
(2014/02/16)
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- PROCESS FOR PREPARATION OF DRONEDARONE BY N-BUTYLATION
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The invention relates to a novel process for preparation of dronedarone (I) and pharmaceutically acceptable salts thereof where the compound of formula (II) or salt thereof is reacted with a compound of formula L-(CH2)3—CH3 (III), where L is a leaving group, and isolating the obtained product and, if desired, converting it into a pharmaceutically acceptable salt thereof. The invention also relates to some novel intermediary compounds and the preparation thereof.
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- Process for preparation of dronedarone by the use of dibutylaminopropanol reagent
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The invention relates to a novel process for preparation of dronedarone of formula (I) and pharmaceutically acceptable salts thereof characterized in that a compound of formula (II) - where L is leaving group - is reacted with compound of formula (III) and the obtained product is isolated and, if desired, converted into a pharmaceutically acceptable salt thereof.
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Paragraph 0044; 0045
(2013/07/31)
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- PROCESS FOR PREPARATION OF DRONEDARONE BY REMOVAL OF HYDROXYL GROUP
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The invention relates to a novel process for preparation of dronedarone of formula (I) and pharmaceutically acceptable salts thereof the hydroxyl group is removed, and the obtained product is isolated and, if desired, converted into a pharmaceutically acceptable salt thereof.
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- PROCESS FOR THE PREPARATION OF DRONEDARONE BY OXIDATION OF A SULPHENYL GROUP
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The invention relates to a novel process for the preparation of dronedarone (I) and pharmaceutically acceptable salts thereof which comprises oxidizing a compound of formula (IV) or a salt thereof with an oxidizing agent in an organic or inorganic solvent or solvent mixture, and isolating the obtained product and, if desired, converting it into a pharmaceutically acceptable salt thereof. Further aspects of the invention include the novel intermediary compound of formula (IV), and a process for the preparation thereof.
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Page/Page column 9; 10
(2013/08/28)
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- Novel Process for the Preparation of Dronedarone
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The subject of the invention is a novel process for the preparation of N-[2-n-butyl-3-{4-[(3-di-n-butylamino)-propoxy]benzoyl}benzofuran-5-yl]-methanesulfonamide of formula I: and pharmaceutically acceptable salts thereof wherein the acyl group of the benzofuran derivative of the general formula II: where R represents C1-4 alkyl-, C1-4 alkoxy- or aryl group, is selectively cleaved and if desired, the resulting compound of formula I is transformed into its salt.
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Paragraph 0052; 0053; 0054; 0055; 0056
(2013/06/04)
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- REDUCTIVE ANIMATION PROCESS FOR PREPARATION OF DRONEDARONE USING ALDEHYDE INTERMEDIARY COMPOUND
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The invention relates to a novel process for preparation of dronedarone of formula (I) and pharmaceutically acceptable salts thereof, characterized in that the compound of formula (II) is reacted with dibutylamine of formula (III), under reducing circumstances, and the obtained product is isolated and, if desired, converted into a pharmaceutically acceptable salt thereof, The invention also relates to some novel intermediary compounds and the preparation thereof.
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- REDUCTIVE AMINATION PROCESS FOR PREPARATION OF DRONEDARONE USING CARBOXYL INTERMEDIARY COMPOUND
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The invention relates to a novel process for preparation of dronedarone of formula (I) and pharmaceutically acceptable salts thereof : Formula (I) characterized in that a compound of formula (II) : Formula (II) is aminated with compound of formula (III) among reductive conditions, : Formula (III) and the obtained product is isolated and, if desired, converted into a pharmaceutically acceptable salt thereof. The invention also relates to some novel intermediary compounds and the preparation thereof.
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- PROCESS FOR PREPARATION OF DRONEDARONE USING AMIDE INTERMEDIARY COMPOUND
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The invention relates to a novel process for preparation of dronedarone of formula (I) and pharmaceutically acceptable salts thereof characterized in that the compound of formula (II) is reduced, and the obtained product is isolated and, if desired, converted into a pharmaceutically acceptable salt thereof. The invention also relates to some novel intermediary compounds and the preparation thereof.
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- METHOD FOR PREPARING 3-KETO-BENZOFURANE DERIVATIVES
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The invention relates to a method for preparing 3-keto-benzofurane derivatives of the general formula: Formula (I), where R is an alkyl or aryl group, R1 is hydrogen or an alkyl or aryl group, and R2 is a substituted alkyl or phenyl group. Said preparation method involves coupling a derivative of Formula III, where X is chlorine, bromine, or iodine or a sulfonate grouping: Formula (III) with a sulfonamide derivative of the formula R—SO2—NH2 in the presence of a basic agent and a catalytic system formed of a complex between a palladium compound and a ligand.
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- PREPARATION PROCESS OF DRONEDARONE AND ITS SALTS
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A process is provided for preparing dronedarone or pharmaceutically acceptable salts thereof. The process comprises reacting 5-amino-2-butyl-3-(4-[3-(dibutylamino)propoxy]benzoyl)benzofuran (compound A) with methanesulfonyl chloride without any catalyst to provide crude dronedarone hydrochloride, which is purified to afford highly pure product. Then, the dronedarone hydrochloride can be converted to highly pure dronedarone through treatment with an alkaline solvent, the dronedarone can be further converted to other pharmaceutically acceptable salts of dronedarone. In this process, acylation between compound A and methanesulfonyl chloride is carried out successfully and the formation of the dimethylsulfonyl by-product is inhibited.
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Paragraph 0058
(2013/03/28)
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- PROCESS FOR PREPARATION OF DRONEDARONE BY GRIGNARD REACTION
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The invention relates to a novel process for the preparation of dronedarone (I) and pharmaceutically acceptable salts thereof, which comprises reacting of compound of formula (IV) with compound of formula (VI) in a Grignard reaction, and the obtained product is isolated and, if desired, converted into a pharmaceutically acceptable salt thereof. The invention also relates to some novel intermediary compounds and processes for the preparation thereof.
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- PROCESS FOR PREPARATION OF DRONEDARONE BY OXIDATION OF A HYDROXYL GROUP
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The invention relates to a novel process for the preparation of dronedarone (I) and pharmaceutically acceptable salts thereof (formula I), which comprises oxidizing a compound of formula (VI), or a salt thereof and the obtained product is isolated and, if desired, converted into a pharmaceutically acceptable salt thereof. Further aspects of the invention include the novel intermediary compound of formula (VI) and process for the preparation thereof.
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Page/Page column 10
(2013/09/12)
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- REDUCTIVE AMINATION PROCESS FOR PREPARATION OF DRONEDARONE USING AMINE INTERMEDIARY COMPOUND
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The invention relates to a novel process for preparation of drohedarone of formula (I) and pharmaceutically acceptable salts thereof characterized in that a compound of formula (II) is reacted in the presence of a reductive agent with butyraldehyde and/or butanoic acid, and isolating the obtained product and, if desired, converting it into a pharmaceutically acceptable salt thereof. The invention also relates to some hovel intermediary compounds and the preparation thereof.
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Page/Page column 18
(2012/10/18)
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- PROCESS FOR PREPARATION OF DRONEDARONE BY N-BUTYLATION
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The invention relates to a novel process for preparation of dronedarone (I) and pharmaceutically acceptable salts thereof where the compound of formula (II) or salt thereof is reacted with a compound of formula L-(CH2)3-CH3 (III), where L is a leaving group, and isolating the obtained product and, if desired, converting it into a pharmaceutically acceptable salt thereof. The invention also relates to some novel intermediary compounds and the preparation thereof.
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- PROCESS FOR PREPARATION OF DRONEDARONE BY MESYLATION
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The invention relates to a novel process for preparation of N-[2-n-butyl-3-[4-[3-(di-n- butylamino)-propoxy]-benzoyl]-benzofuran÷5-yl]methanesulfonamide (I) and pharmaceutical acceptable salts thereof, where a salt of (5-amino-2-butyl-l- berizofuran-3-yl){4-[3-(di-n-butylamino)propoxy]phenyl}methanone of formula (II) - where A is a mono- or dibasic acid forming an acid addition salt with the compound of formula (II), n is 1 if A is dibasic acid and n is 1 or 2 if A is a monobasic acid - is reacted with a mesylating reagent in a heterogen reaction, if desired, in the presence of a phase transfer catalyst. The invention also relates to the novel salts of compound of formula (II), for the preparation thereof and their use in the preparation of dronedarone.
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Page/Page column 12-13
(2012/10/18)
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- An improved scalable route to pure dronedarone hydrochloride
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An efficient scalable synthesis for dronedarone hydrochloride (2) via Friedel-Craft acylation of 2-(-2-butyl-1-benzofuran-5-yl)-1H-isoindole-1,3(2H) dione (12) with 4-(3-chloropropoxy) benzoic acid (13) in good yield and high purity has been developed by using Eaton's reagent instead of hazardous and toxic metal halide catalyst like AlCl3 or SnCl4.
- Hivarekar, Raghvendra R.,Deshmukh, Sanjay S.,Tripathy., Narendra K.
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p. 677 - 681
(2012/08/07)
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- PROCESS FOR THE PREPARATION OF 3-AROYL-5-AMINOBENZOFURAN DERIVATIVES
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The present invention relates to a process for the preparation of 3-aroyl -5- aminobenzofuran derivatives useful as antiarrhythmic drugs which avoids the use of nitro intermediates.
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- Process for the preparation of 3-aroyl-5-aminobenzofuran derivatives
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The present invention relates to a process for the preparation of 3-aroyl-5-aminobenzofuran derivatives useful as antiarrhythmic drugs which avoids the use of nitro intermediates.
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- NOVEL PROCESS FOR THE PREPARATION OF DRONEDARONE
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The subject of the invention is a novel process for the preparation of N-[2-n-butyl-3-{4-[(3-di-n-butylamino)- propoxy]benzoyl}benzofuran-5-yl]-methanesulfonamide of formula (I), and pharmaceutically acceptable salts thereof characterized in that, the acyl group of the benzofuran derivative of the general formula (II), where R represents C 1-4 alkyl-, C1-4 alkoxy- or aryl group - is selectively cleaved and if desired, the resulting compound of formula I is transformed into its salt.
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Page/Page column 12
(2012/02/05)
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- PROCESSES FOR PREPARING DRONEDARONE AND ITS INTERMEDIATES
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The invention relates to process for the preparation of benzofuran derivative and intermediates thereof. More particularly, it relates to processes for the preparation of dronedarone or pharmaceutically acceptable acid addition salts thereof in crystalline form. The invention also relates to pharmaceutical compositions that include the dronedarone hydrochloride in crystalline form substantially free from disulfonamide impurity.
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Page/Page column 36
(2012/03/27)
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- PROCESS FOR OBTAINING DRONEDARONE
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The present invention provides a process for obtaining dronedarone or salts thereof characterized in that in an organic phase comprising one or more non-polar solvents, 5-amino-3-[4-(3-di-n-butylaminopropoxy)benzoyl]-2-n-butyl-benzofuran is reacted with methane sulfonyl chloride without the addition of a base. The invention also provides a process for obtaining intermediates of dronedarone environmentally friendly and industrially viable.
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Page/Page column 13
(2012/05/05)
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- Process for obtaining dronedarone
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The present invention provides a process for obtaining dronedarone or salts thereof characterized in that in an organic phase comprising one or more non-polar solvents, 5-amino-3-[4-(3-di-n-butylaminopropoxy)benzoyl]-2-n-butyl-benzofuran is reacted with methane sulfonyl chloride without the addition of a base. The invention also provides a process for obtaining intermediates of dronedarone environmentally friendly and industrially viable..
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Page/Page column 9
(2012/05/20)
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- PROCESS FOR PREPARING DRONEDARONE
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Disclosed is a process for preparing dronedarone and pharmaceutically acceptable salts thereof. Also disclosed are a novel amorphous form of dronedarone hydrochloride and a preparation process thereof.
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Page/Page column 20-21
(2012/02/02)
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- IMPROVED PROCESSES FOR OBTAINING HIGH PURITY OF DRONEDARONE HYDROCHLORIDE
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Improved processes for obtaining high purity of Dronedarone hydrochloride (chemically known as N-(2-buty1-3-(4-(3-(dibutylamino)propoxy)benzoyl)-5-benzofuranyl)methanesulfonamide hydrochloride) are provided.
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Page/Page column 3; 13
(2012/12/13)
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- Synthesis of dronedarone and salts thereof
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The present invention relates to a process for preparation of Dronedarone or pharmaceutically acceptable salts thereof. More particularly, the present invention provides a process for preparation of Dronedarone hydrochloride, without the isolation of Dronedarone base.
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Page/Page column 11-12
(2012/03/27)
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- PROCESS FOR PREPARATION OF N-[2-BUTYL-3-[4-[3-(DIBUTYLAMINO)PROPOXY]BENZOYL]-5-BENZOFURANYL]METHANESULFONAMIDE, ACID ADDITION SALTS AND PRODUCT THEREOF
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The present invention relates to a process for the preparation of highly pure N-[2- butyl-3-[4-[3-(dibutylamino)propoxy]benzoyl]-5- benzofuranyljmethanesulfonamide and pharmaceutically acceptable salts thereof having HPLC purity greater than 99.5%.
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Page/Page column 20-21
(2012/02/01)
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- SYNTHESIS OF DRONEDARONE AND SALTS THEREOF
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The present invention relates to a process for preparation of Dronedarone or pharmaceutically acceptable salts thereof. More particularly, the present invention provides a process for preparation of Dronedarone hydrochloride, without the isolation of Dronedarone base.
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Page/Page column 8
(2012/05/07)
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- PROCESS FOR THE PREPARATION OF DRONEDARONE
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This invention relates to a process for the preparation of N-[2-n-butyl-3-{4-[(3- dibutylamino)-propoxy]-benzoyl} - 1-benzofuran-5-yl]-methane-sulfonamide of formula (I) and its pharmaceutically acceptable salts, according to one of the methylsulfonyl groups of the 2-n-butyl-3-[(di-n-butylamino-3-propoxy)-benzoyl]-5- bis-(methylsulfonamido)-benzofuran of formula (II) is selectively cleaved and if desired, the resulting compound of formula (I) is transformed into its salt.
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Page/Page column 11
(2012/01/06)
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- PREPARATION OF BENZOFURANS AND USE THEREOF AS SYNTHETIC INTERMEDIATES
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The present invention provides several synthetic methods for preparing N-(2-butylbenzofuran-5-yl)-N-(methylsulfonyl)methanesulfonamide, a compound of formula (3), an intermediate in the preparation of Dronedarone. The present invention further provides a process for preparing Dronedarone, comprising the steps of converting 2-butyl-5-bis(methanesulfon)-amidobenzofuran of formula (3) to Dronedarone, wherein the 2-butyl-5-bis(methanesulfon)-amidobenzofuran of formula (3) is prepared by the processes of the present invention.
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Page/Page column 42
(2011/09/15)
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- Process for preparing dronedarone
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The present invention relates to a process for preparing dronedarone and in particular for preparing an intermediate useful in the preparation of dronedarone. Furthermore, the present invention relates to a process for preparing crystalline dronedarone hydrochloride as well as pharmaceutical compositions comprising this salt.
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- Crystalline dronedarone salts
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The present invention relates to crystalline dronedarone salts, a process for their preparation as well as pharmaceutical compositions comprising these salts.
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Page/Page column 9
(2011/10/13)
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- NEW PROCESS FOR THE PREPARATION OF DRONEDARONE
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The subject of the present invention is a novel process for the preparation of N- [2-n-butyl-3-{4-[(3-dibutylamino)propoxy]benzoyl}-1-benzofuran-5- yl] methanesulfonamide of formula (I) and the new intermediates of the reparation process.
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Page/Page column 8
(2011/08/03)
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- Crystallized form of dronedarone base
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The invention relates to a novel crystallized form of dronedarone base, to its process of preparation and to the pharmaceutical compositions containing said novel crystallized form.
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Page/Page column 7
(2011/09/12)
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- NEW PROCESS FOR THE PREPARATION OF DRONEDARONE
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The subject of the present invention is a novel process for the preparation of N- [2-n-butyl-3-{4-[(3-dibutylamino)propoxy]benzoyl}-1-benzofuran-5- yl] methanesulfonamide of formula (I) and the new intermediates of the preparation process.
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- 2-butyl-3-(4-[3(dibutylamino)propoxy]benzoyl)-5-nitro-benzofuran hydrochloride and preparation thereof
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The invention relates to 2-butyl-3-(4-[3-(dibutylamino)propoxy]benzoyl-5-nitrobenzofuran hydrochloride, to its preparation and to its use as synthetic intermediate, in particular in preparing 2-butyl-3-(4-[3-(dibutylamino)propoxy]benzoyl)-5-nitrobenzofuran, itself an intermediate for dronedarone.
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Page/Page column 6
(2008/06/13)
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- Methanesulphonamido-benzofuran, preparation method and use thereof as synthesis intermediate
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The invention relates to 2-butyl-5-(methanesulfonamido)benzofuran, its preparation and its use. This compound is a synthesis intermediate, in particular for the preparation of dronedarone.
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Page/Page column 5
(2008/06/13)
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- Alkylaminoalkyl derivatives of benzofuran, benzothiophene, indole and indolizine, process for their preparation and compositions containing them
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The subject of the invention is benzofuran, benzothiophene, indole or indolizine compounds of general formula: STR1 in which: Het represents one of the groups: STR2 in which T,T' and T"represent particularly a group: STR3 R and Ra, identical or different, represent X represent --O-- or --S-- Y represents a radical STR4 These compounds are useful as medecines particularly for the treatment of pathological syndroms of the cardio-vascular system.
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