- Iodine/persulfate-promoted site-selective direct thiolation of quinolones and uracils
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A simple and general method for direct thiolation of 4-quinolones with disulfides or thiols under I2/K2S2O8 system has been developed. Under the optimal conditions, the C–S bond coupling can take place effectively with good to decent yields and excellent regioselectivity of the S-linked products. The established metal-free site-selective approach was also applicable to transform a range of uracil substrates to the thio-substituted products under mild conditions. Further transformation to the sulfone derivatives can be conveniently performed in one-pot. These easy-to-handle protocols represent a useful and interesting synthetic alternative with good substrate scope and functional group compatibility.
- Beukeaw, Danupat,Noikham, Medena,Yotphan, Sirilata
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supporting information
(2019/09/03)
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- Doxofylline impurity and preparation method thereof
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The invention provides a doxofylline impurity and a preparation method thereof. The impurity is 9-(2,2-dimethoxyethyl)-1,3-dimethyl-1H-purine-2,6(3H,9H)-diketone. A compound provided by the inventioncan be used as a standard substance for detecting ingredients of a doxofylline finished product, thereby improving the accurate positioning and characterization of the detection and analysis of doxofylline finished product for the impurities, strengthening the control of the impurities, and further improving the quality of the doxofylline finished products.
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Paragraph 0020-0024
(2019/05/22)
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- Pd/PTABS: Catalyst for Room Temperature Amination of Heteroarenes
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A mild and highly efficient catalytic amination procedure for chloroheteroarenes at ambient temperature using the Pd/PTABS catalytic system is reported. The protocol is selective for the amination of chloroheteroarenes using secondary amines such as piperidine, pyrrolidine, and several others. The exceptional mildness of the developed protocol is beneficial for the synthesis of a crucial Buparlisib intermediate as well as the formal synthesis of Alogliptin in competitive yields.
- Murthy Bandaru, Siva Sankar,Bhilare, Shatrughn,Chrysochos, Nicolas,Gayakhe, Vijay,Trentin, Ivan,Schulzke, Carola,Kapdi, Anant R.
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supporting information
p. 473 - 476
(2018/01/28)
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- A natural product four methyl uric acid fully synthetic method
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The invention relates to a total synthesis method for a natural product tetramethyl uric acid. The method comprises the following steps: (1) using 1,3-dimethyl barbituric acid as a raw material for synthesis to obtain an intermediate 6-substitued-1,3-dimethyl pyrimidine-2,4-diketone; (2) synthesizing an intermediate 1,3-dimethyl-6-methylamino pyrimidine-2,4-diketone; (3) synthesizing an intermediate 1,3-dimethyl-5-substitued-6-methylamino pyrimidine-2,4-diketone; (4) synthesizing an intermediate 1,3-dimethyl-5,6-dimethylamino pyrimidine-2,4-diketone; (5) synthesizing a target compound 1,3,7,9-tetramethyl uric acid. The method is convenient for synthesis, has a higher yield, and can ease the demand on tetramethyl products to a certain degree.
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Paragraph 0033; 0034; 0035
(2017/08/25)
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- ETHYNYLXANTHINES, PREPARATION AND USE AS CALCIUM ION CHANNEL MODULATORS
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The present invention relates to novel pharmaceutical compounds, which exhibit ability to act as calcium ion channel modulators, methods for their synthesis and the treatment and/or prevention of various diseases and disorders including deregulated calcium ion channel activity.
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Page/Page column 12; 13
(2016/10/27)
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- AMIDES OF 2-AMINO-4-ARYLTHIAZOLE COMPOUNDS AND THEIR SALTS
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The present disclosure is directed to salts of N-{4-[2,4-difluoro-3- (trifluoromethyl)phenyl]-1,3-thiazol-2-yl}-2-(1,3-dimethyl-2,4-dioxo-1,2,3,4- tetrahydrothieno[2,3- d]pyrimidin-5-yl)acetamide and process for the preparation thereof (formula II)..
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Page/Page column 64
(2014/01/08)
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- AMIDES OF HETEROCYCLIC COMPOUNDS AS TRPA1 INHIBITORS
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Amides of heterocyclic compounds as Transient Receptor Potential subfamily A (TRPA) modulators are provided In particular, compounds described herein are useful for treating or preventing diseases, conditions and/ or disorders modulated by TRPA1 (Transient Receptor Potential subfamily A, member 1) Also provided herein are processes for preparing compounds described herein, intermediates used in their synthesis, pharmaceutical compositions thereof, and methods for treating or preventing diseases, conditions and/or disorders modulated by TRPA1. (I).
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Page/Page column 48
(2011/10/10)
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- Enantioconservative synthesis of polysubstituted pyrimido[4,5- b ]azepines
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A three-step enantioconservative protocol was developed for the synthesis of polysubstituted pyrimido[4,5-b]azepines. First, 1,3-dimethyl-6-[N-(2- alkoxycarbonylalkyl)amino]uracils were synthesized by nucleophilic substitution of 6-chloro-1,3-dimethyluracil with amino acids. Subsequent acylation of the uracils by a mixture of acetic anhydride and cyanoacetic acid gave the corresponding 5-cyanoacetylated pyrimidines. In the final step, the pyrimidines were subjected to Dieckmann cyclization with a sodium alcoholate in the corresponding alcohol to afford the corresponding pyrimido[4,5-b]azepines. By using uracils of N-monosubstituted amino acids, cyclization was combined with ring opening of the pyrimidine ring system to afford polysubstituted azepines. Georg Thieme Verlag Stuttgart.
- Gerig, Britta,Girreser, Ulrich,Schuett, Martin,Heber, Dieter
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body text
p. 2017 - 2022
(2010/08/22)
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- FUSED PYRIMIDINE-DIONE DERIVATIVES AS TRPA1 MODULATORS
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The invention described herein relates to novel fused pyrimidinediones derivatives of formula (I) which are TRPA (Transient Receptor Potential subfamily A) modulators. In particular, compounds described herein are useful for treating or preventing diseases, conditions and/or disorders modulated by TRPAl (Transient Receptor Potential subfamily A, member 1). This invention also provides processes for preparing compounds described herein, intermediates used in their synthesis, pharmaceutical compositions thereof, and methods for treating or preventing diseases, conditions and/or disorders modulated by TRPAl. Formula (I)
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Page/Page column 33
(2010/11/03)
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- PYRIMIDINEDIONE-FUSED HETEROCYCLIC COMPOUNDS AS TRPA1 MODULATORS
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The present invention is related to novel pyrimidinedione-fused heterocyclic compounds as TRPA (Transient Receptor Potential subfamily A) modulators. In particular, compounds described herein are useful for treating or preventing diseases, conditions and/or disorders modulated by TRPA1 (Transient Receptor Potential subfamily A, member 1). Also provided herein are processes for preparing compounds described herein, intermediates used in their synthesis, pharmaceutical compositions thereof, and methods for treating or preventing diseases, conditions and/or disorders modulated by TRPA1.
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Page/Page column 41
(2010/11/17)
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- A mild and efficient method for the deformylation of 5-formyl uracils and synthesis of 4,4￠-methylidenebis(1-phenyl-3-methyl-5-pyrazolone)
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6-Substituted 5-formyl uracils undergo an interesting reaction with 1-phenyl-3-methyl-5-pyrazolone in the presence of base catalyst to afford deformylated uracils and 4,4￠-methylidenebis(1-phenyl-3-methyl-5- pyrazolone) in excellent yields. Georg Thieme V
- Deb, Mohit L.,Majumder, Swarup,Bhuyan, Pulak J.
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scheme or table
p. 1982 - 1984
(2010/03/26)
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- Synthesis of pyrimidine derivatives possessing an antioxidative property and their inhibitory effects on picryl chloride-induced contact hypersensitivity reaction
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We conducted a preliminary structure-activity relationship (SAR) study of some barbituric acid and uracil derivatives against the picryl chloride-induced contact hypersensitivity reaction. The introduction of an antioxidative moiety to the side chain of the C(6)-position of uracil was effective against this model. The introduction of dimethoxyphenol (8b) or dimethylphenol (8c) instead of di-t-butylphenol (8a) as an antioxidative moiety gave diminished activities, so, the reactive oxygen would contribute to the inflammation of this model, and an antioxidative activity was required for exhibiting the inhibitory activity. The inhibitory activity was significantly affected by the substituent at the N(1)-phenyl moiety.
- Isobe, Yoshiaki,Hirota, Kosaku
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p. 1451 - 1454
(2007/10/03)
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- Studies on uracils: An efficient method for the synthesis of novel 1-alIyl-6-(1′,2′,3′-triazolyl) analogues of KEPT
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An efficient synthetic method for preparing novel l-aIlyl-6(1′,2′,3′-triazolyl) analogues of KEPT, an anti-HIV reverse transcriptase inhibitor, is reported. The key step is based upon selective intermolecular cycloaddition of azide to acetylenes. The Royal Society of Chemistry 1999.
- Bhuyan, Pulak J.,Borah, Harsha N.,Sandhu, Jagir S.
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p. 3083 - 3084
(2007/10/03)
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- Synthesis of amphiphilic 8-decyl-1,3,6,7-tetramethyl-7,8-dihydropterine-2,4-dione
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The condensation of 5-amino-6-decylamino-1,3-dimethyluracil with 2,3-butanedione in the presence of 1N HCl gives 5N-(1'-acetyl-1'-methylmethylene)-6N-decylamino-1,3-dimethyluracil which cyclises to amphiphilic 8-decyl-1,3,6,7-tetramethyl-7,8-dihydropterine-2,4-dione (5) in the presence of 12 N HCl.
- Chauhan, S. M. S.,Tomar, Jaya,Gupta, M.
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p. 869 - 871
(2007/10/03)
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- PURINES AND PYRIMIDINES AND CONDENSED SYSTEMS BASED ON THEM. 2. SYNTHESIS OF 1-METHYL-9-AMINOXANTHINE AND 9-AMINOTHEOPHYLLINE
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The previously unknown 9-aminotheophylline and 1-methyl-9-aminoxanthine were synthesized from 3-methyl-5-amino-6-hydrazinouracil.In the case of 1-methyl-9-aminoxanthine an x-ray diffraction study of an N-amino derivative of an NH heterocycle was made for the first time.
- Kuz'menko, V. V.,Kuz'menko, T. A.,Aleksandrov, G. G.,Pozharskii, A. F.,Gulevskaya, A. V.
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p. 690 - 697
(2007/10/02)
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- Alkylation des pyrimidines en catalyse par transfert de phase
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Nous rapportons ici, la premiere etude concernant l'alkylation simple et efficace, en catalyse par transfert de phase, de dianions pyrimidiques ambidents derives de l'uracile, de la thymine, du nitro-5 uracile, du fluoro-5 uracile, du chloro-6 uracile, de la tetrahydro-1,2,3,4 dioxo-2,4 quinazoline, conduisant selectivement et avec de hauts rendements, aux derives N1,N3-dialkyles correspondants.
- Hedayatullah, Mir
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p. 339 - 342
(2007/10/02)
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