发明名称 THIOCARBAMOYLTHIO FATTY ACID DERIVATIVES
摘要 This invention relates to novel compounds of the general formula (I) , wherein R1 and R2 each independently represent a hydrogen or halogen atom or a methyl, methoxy or pchlorophenoxy group, at least one of R1 and R2 being other than hydrogen, Y represents a cyano group or a group of the formula in which R3 represents a hydroxy, lower alkoxy or hydroxy-(lower alkoxy) group or a group of the formula -N(R4)(R5) group in which R4 represents a hydrogen atom and R5 represents a cycloalkyl group containing up to 6 carbon atoms or R4 and R5 each independently represent a hydrogen atom or a lower alkyl group or R4 and R5 together with the nitrogen atom to which they are attached represent a piperidine or morpholine ring, A represents a methylene, ethylene, propylene or -OCH2CH2- group and n stands for an integer of from 2 to 10 inclusive, and salts of acids of formula I with bases. These compounds and salts have blood-fat lowering activity. They can be prepared by a process which comprises reacting a compounds of the general formula (II) , wherein R1, R2 and A have the significance given in claim 1 and M+ represents Na , K+ or NH4+, with a compound of the general formula X(CH2)nY (III) , wherein X represents a halogen atom and Y and n have the significance given above, or with an alkali metal salt of a halocarboxylic acid of the general formula X(CH2)nCOOH (IV) wherein X and n have the significance given earlier in this claim, or reacting an isothiocyanate of the general formula (V) , wherein R1, R2 and A have the significance given above, with a mercaptan of the general formula HS - (CH2)n - Y (VI) , wherein Y and n have the significance given above, and, if desired, saponifying an ester obtained or an amide obtained to an acid, re-esterifying an ester obtained, esterifying an acid obtained or converting same into a salt with a base, hydrolysing a nitrile obtained to an amide or dehydrating an amide obtained to a nitrile.
申请公布号 AU2513977(A) 申请公布日期 1978.11.16
申请号 AU19770025139 申请日期 1977.05.13
申请人 HOFFMANN-LA ROCHE, F. & CO. A.G. 发明人 ULF FISCHER;ADO KAISER
分类号 C07C333/20;A61K31/27;A61K31/40;A61P3/06;C07C67/00;C07C325/00;C07D295/185 主分类号 C07C333/20
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