- Preparation method of phenyl-containing compound
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The present invention discloses a method for preparing an phenyl-containing compound. The present invention provides a method for preparing a compound shown in formula I, comprising the following steps: in the presence of formamide or acetamide, in the pr
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Paragraph 0090-0098
(2022/01/04)
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- Preparation method of chiral aromatic cyclopropylamine and salt thereof and intermediate used in preparation method
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The embodiment of the invention provides a preparation method of a compound as shown in a formula I or salt thereof, which comprises the following steps: (1) reacting a compound as shown in a formulaVI with a compound as shown in a formula VII in a first
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- Preparation method of ticagrelor key intermediate aromatic cyclopropanamide
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The invention discloses a preparation method of a ticagrelor key intermediate, aromatic cyclopropanamide. The method comprises the following steps: with (1R,2R)-2-(3,4-difluorophenyl)-1-cyclopropyl formate (I) as an initial raw material, carrying out tran
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Paragraph 0028-0034
(2019/11/20)
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- Synthetic method for ticagrelor intermediate (1R,2S)-2-(3,4-difluorophenyl)cyclopropylamine
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The invention discloses a synthetic method for a ticagrelor intermediate (1R,2S)-2-(3,4-difluorophenyl)cyclopropylamine. The method comprises the following steps: (5H)-furan-2-one is taken as a starting raw material, the (5H)-furan-2-one and a 3,4-difluor
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- Preparation method of ticagrelor
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The invention discloses a preparation method of ticagrelor. The preparation method comprises the following steps: (1) preparation of ticagrelor intermediate product 1-TK acid; (2) preparation of ticagrelor intermediate product 2-TK-amide; (3) preparation of ticagrelor intermediate product 3-TK-amino compound hydrochloride; (4) preparation of ticagrelor intermediate product 4-TK-amino compound R-tartrate; ( 5) preparation of ticagrelor intermediate product 5-TK-amino compound L-mandelate; and (6) preparation of ticagrelor-TK. The preparation method has the advantages of cost advantage, mature and stable process, stable product quality, and safe and reliable production process.
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Paragraph 0035; 0045; 0047; 0049; 0089; 0130
(2018/04/21)
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- Synthetic method of ticagrelor intermediate and intermediate thereof
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The invention discloses a synthetic method of a ticagrelor intermediate and the intermediate thereof. The synthetic method comprises the following steps of: firstly, performing a diazo-reaction on a compound (2) to prepare a compound (3); performing a rho
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Paragraph 0043-0045; 0058
(2017/07/21)
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- for standard auspicious Luo river intermediate preparation method
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The inventiondiscloses a preparation method of ticagrelor. The method comprises the following steps: (1) reducing a compound shown in a formula III in the presence of a proton source provided by sodium borohydride or potassium borohydride and diethyl aniline hydrochloride to obtain a compound shown in a formula IV; (2) reacting the compound IV in the presence of alkali to generate a compound VI; (3) hydrolyzing the compound VI without purification to generate a compound VII; (4) reacting the compound VII to generate acyl chloride, reacting the acyl chloride to generate formamide, thus obtaining a compound shown in a formula IX; and (5) carrying out Hofmann rearrangement on the compound IX to obtain a compound shown in a formula II. Regents used in the method are nontoxic, harmless, environmentally friendly and low in price; the used key reagents can be recycled. Therefore, the method is applicable to industrial production.
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Paragraph 0082; 0083
(2017/08/25)
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- (1 R, 2 S) - 2 - (3, 4 - difluorophenyl) amine ·D - mandelic acid salt preparation method
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The invention discloses a preparation method of (1R,2S)-2-(3,4-difluorophenyl) rolicyprine.D-mandelate. The preparation method comprises the following steps: carrying out cyclopropanation on a compound shown in a formula V to obtain a compound shown in a formula IV; carrying out amide generation and Hofmann degradation to obtain a compound shown in a formula II; and performing salification with D-mandelic acid to obtain a compound shown in a formula I. The compound shown in the formula V is prepared in a way that a compound shown in a structure formula VI is subjected to CBS asymmetric reduction reaction, wherein a catalyst for the CBS asymmetric reduction reaction is a compound shown in a structural formula VII, and a reduction agent for the CBS asymmetric reduction reaction can be borane-tetrahydrofuran or borane-N,N-diethyl phenylamine.
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Paragraph 0119-0122
(2018/02/04)
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- Intermediate for standard auspicious Luo river (1R, 2S) - 2 - (2,3-difluorophenyl) method for the preparation of cyclopropylamines (by machine translation)
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The invention discloses a method for preparing ticagrelor midbody (1R,2S)-2-(2,3-difluorophenyl) cyclopropylamine, belonging to the technical fields of organic synthesis route design and preparation of raw material medicines and midbodies. The method comprises the following steps: performing alcoholysis on succinic anhydride, thereby obtaining mono-methyl succinate, performing acylating chlorination reaction on mono-methyl succinate, thereby obtaining a compound methyl 4-chloro-4-oxobutyrate, performing Fridel-Crafts reaction on methyl 4-chloro-4-oxobutyrate and o-difluorobenzene, thereby obtaining a compound methyl 4-ketone-4-(3,4-difluorophenyl) butyrate (IV), and further performing asymmetric reduction reaction, cyclization reaction and Hoffman degradation on the compound IV, thereby obtaining the compound (1R,2S)-2-(2,3-difluorophenyl) cyclopropylamine. Initial raw materials used in the method are low in cost and easy to obtain, the reaction condition is gentle, the operation is safe, simple and convenient, the environment pollution is small, and the key ticagrelor midbody prepared by using the method is simple and convenient in after treatment, and is beneficial to on-scale production.
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Paragraph 0037; 0062; 0068
(2017/03/23)
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- Biocatalytic approaches to a key building block for the anti-thrombotic agent ticagrelor
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Three complementary biocatalytic routes were examined for the synthesis of the cyclopropyl amine (1R,2S)-2, which is a key building block for the anti-thrombotic agent ticagrelor 1. By employing either a ketoreductase, amidase or lipase biocatalyst, the k
- Hugentobler, Katharina G.,Sharif, Humera,Rasparini, Marcello,Heath, Rachel S.,Turner, Nicholas J.
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supporting information
p. 8064 - 8067
(2016/09/09)
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- An important intermediate for card Grey (1R, 2S) - 2 - (3,4-di-fluorophenyl) method for the preparation of cyclopropylamines
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The invention relates to a method for preparing important midbody (1R,2S)-2-(3,4-difluorinated phenyl) cyclopropylamine of ticagrelor. The method mainly comprises the following steps: performing cyclopropane reaction on camphor sulfonium ylide I and acryl
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Paragraph 0043; 0044
(2016/10/08)
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- Synthesizing method of (1R,2S)-2-(3,4-difluorophenyl)cyclopropylamine
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The invention provides a synthesizing method of (1R,2S)-2-(3,4-difluorophenyl)cyclopropylamine. The synthesizing method comprises the steps that a compound (I) reacts with diethyl cyanomethylphosphonate in the presence of alkaline substances to obtain a c
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Paragraph 0055; 0056
(2017/02/28)
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- Synthesis and biological evaluation of ticagrelor derivatives as novel antiplatelet agents
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Ticagrelor (1) is the first reversible P2Y12 receptor antagonist blocking adenine diphosphate (ADP)-induced platelet aggregation with rapid onset and offset of effects. In this study, synthesis of ticagrelor and its derivatives has been accomplished in a convergent way. The compound design was based on modifications of ticagrelor and its major metabolite (33) in order to ameliorate their pharmacokinetic properties and dosing profile. The final compounds (1a-g, 35a-g) were evaluated for their inhibitory effect on ADP-induced platelet aggregation in rats. The assay results showed that some compounds (e.g., 1b, 1d, 33, 35b, 35f) exhibited comparable potency with that of ticagrelor.
- Zhang, Hao,Liu, Jun,Zhang, Luyong,Kong, Lingyi,Yao, Hequan,Sun, Hongbin
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p. 3598 - 3602
(2012/07/14)
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- CHEMICAL PROCESS FOR PREPARATION OF AROMATIC CYCLOPROPANE ESTERS AND AMIDES
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The present invention relates to compounds useful as pharmaceutical intermediates, to processes for preparing said intermediates, to intermediates used in said processes, and to the use of said intermediates in the preparation of pharmaceuticals. In particular, the present invention concerns enantiomerically pure trans-cyclopropane carboxylic acid derivatives, processes for preparing said carboxylic acid derivatives and their use in preparing pharmaceuticals.
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Page/Page column 7-8
(2008/06/13)
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- A PROCESS FOR THE PREPARATION OF OPTICALLY ACTIVE CYCLOPROPYLAMINES
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This invention relates to a process for the production of optically active 2-(disubstituted aryl) cyclopropylamine derivatives and optically active 2-(disubstituted aryl) cyclopropane carboxamide derivative which are useful intermediates for the preparati
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Page/Page column 31
(2008/06/13)
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