- Pyrrole imidazole ring derivative and medical use thereof wherein the compound represented by the general formula (I) has excellent inhibitory effect on and selectivity of dipeptidyl peptidase IV(DPP-IV)
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The present invention relates to a pyrrole imidazole ring derivative and medical use thereof, more particularly a pyrrole imidazole ring derivative represented by the general formula (I) or stereoisomers thereof, pharmaceutically acceptable salts thereof, prodrugs, pharmaceutical compositions containing the derivative, and pharmaceutical applications for the preparation of dipeptidyl peptidase IV(DPP-IV) inhibitors, wherein the definitions of all substitution groups in general formula (I) are the same as those defined in the specification.
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Page/Page column 65; 66
(2017/08/02)
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- Pyran derivative salt or its salt hydrate and its preparation and use (by machine translation)
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The invention relates to a benzopyran derivative salt or its salt hydrate and its preparation and application, and in particular relates to dipeptide kinase - IV inhibitor a pharmaceutically acceptable salt or its salt hydrate, and its preparation method and application, further for the purposes of formula (I) as shown in the salt or its salt hydrate and its preparation method and application. (by machine translation)
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Paragraph 0108; 0109; 0110; 0111; 0112; 0113; 0114; 0115
(2017/08/29)
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- Chemoenzymatic method of 1,2,4-triazole nucleoside synthesis: Possibilities and limitations
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Possibilities and limitations of chemoenzymatic synthesis of novel structural analogues of an antiviral preparation of Ribavirin (1-β-D-ribofuranosyl-1,2,4-triazole-3-carboxamide) were established. A synthesis of various amides of 1H-1,2,4-triazole-3-carboxylic acid and its 5-substituted analogues - potential substrates of purine nucleoside phosphorylase - has been described. Comparative efficiency of preparation methods of these amides, as well as the methods of introduction of functional groups to the C5 position of heterocyclic system, were investigated. Novel analogues of Ribavirin containing various substitutes in the carboxamide group were synthesized. A biotechnological method was developed for the preparation of 1-β-D-ribofuranozyl-1,2,4-triazole-3-carbonitryl, an intermediate in the synthesis of Viramidine, the modern analogue of Ribavirin.
- Konstantinova,Chudinov,Fateev,Matveev,Zhurilo,Shvets,Miroshnikov
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- NOVEL PROCESSES FOR THE PREPARATION OF SUBSTITUTED PROPENONE DERIVATIVES
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The present invention provides industrial and commercial processes for the preparation of 2-acyl-5-benzylfuran derivatives, 1,2,4-triazole-3-carboxylic acid ester derivatives and propenone derivatives having anti-HIV activities and usuful crystals thereof. wherein R1, R2 and R4 each is independently hydrogen or the like; A is CR6 or N; R6 is hydrogen or the like; Q is a protecting group; and L is a leaving group.
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- A practical synthesis of ethyl 1,2,4-triazole-3-carboxylate and its use in the formation of chiral 1',2'-seco-nucleosides of ribavirin
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A practical and efficient synthesis of ethyl 1,2,4-triazole-3-carboxylate (6a, R'' = H) from ethyl carboethoxyformimidate hydrochloride is described. Alkylation of this heterocycle with the chloromethyl ethers of 1,3-O-dibenzylbutane-1,2R,3S-triol and 1,3
- Vemishetti,Leiby,Abushanab,Panzica
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p. 651 - 654
(2007/10/02)
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- Purines, Pyrimidines, and Imidazoles. Part 58. Synthesis and Reactions of some Imidazole-2,4-dicarboxylic Acid Derivatives
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Diethyl 5-amino-1-(p-methoxybenzyl)imidazole-2,4-dicarboxylate (3b) has been prepared from ethyl 2-amino-2-cyanoacetate and ethyl 1-ethoxycarbonylformimidate hydrochloride or ethyl triethoxyacetate followed by reaction with p-methoxybenzylamine.The diester, with one equivalent of dilute sodium hydroxide solution, furnished ethyl 5-amino-1-(p-methoxybenzyl)imidazole-4-carboxylate (7a).Diazotisation of the diester (3b) and reaction of the diazonium salt with copper(I) chloride produced diethyl 5-chloro-1-(p-methoxybenzyl)imidazole-2,4-dicarboxylate (9a) which, with dilute alkali, gave ethyl 5-chloro-1-(p-methoxybenzyl)imidazole-4-carboxylate (7b).Diazotisation of the diester (3b) in the presence of hypophosphorous acid gave diethyl-1-(p-methoxybenzyl)imidazole-2,4-carboxylate (9b) which, when hydrogenated over palladium-charcoal, produced diethyl imidazole-2,4-dicarboxylate (9c).This with bromine (chlorine) gave diethyl 5-bromo(chloro)imidazole-2,4-dicarboxylate (9d and e).The chloro derivative (9a) was similarly hydrogenated using palladium-charcoal to produce diethyl 5-chloroimidazole-2,4-dicarboxylate (9e).
- Brown, Tom,Shaw, Gordon,Durant, Graham J.
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p. 809 - 812
(2007/10/02)
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