PROCEDEU PENTRU PREPARAREA SULFONILAMINOPIRIMIDINELOR

摘要

1346705 Sulphonylaminopyrimidines BOEHRINGER MANNHEIM GmbH 16 Oct 1972 [20 Oct 1971] 47608/72 Heading C2C Novel sulphonylaminopyrimidines of Formula where A is a bicyclic oxygen or sulphur containing heterocycle, optionally substituted by halogen, C 1 -C 3 alkyl and/or C 1 -C 3 alkoxy groups; Y is a C 1 -C 3 alkylene; R 1 is H or together with Y represents a C 3 or C 4 carbon bridge; R 2 is alkyl, cycloalkyl, cycloalkylalkyl, alkoxy, cycloalkoxy, alkoxyalkyl, alkoxyalkoxy, alkythio, alkythioalkyl, phenyl or benzyl; R 3 is hydrogen or C 1 -C 5 alkyl; or R 2 and R 3 together form a C 3 -C 5 methylene chain, and the physiologically compatible salts thereof maybe prepared by reacting (a) a compound of general Formula II with a reactive derivative of an acid of formula ACO 2 H, (b) a compound of Formula III wherein n = 0, 1 or 2, with a compound of Formula IV followed, if necessary by oxidation to the sulphonamide, (c) a compound of Formula V with a compound of formula where Z and Z1 which may be the same or different are H or alkoxy; or with an enamine or acetal thereof, whereafter when the product is hydroxylated in the 4- and/or 6-position it is first converted to the corresponding halogen compound and thereafter reductively dehalogenated to the pyrimidine, or (d) a compound of Formula VI with a compound of Formula VII wherein T is a halogen atom or a trialkylammonio group in which the alkyl groups have 1-5 carbon atoms. 5 - Methoxy - 2 - methyl - 2,3 - dihydrobenzo- [b]-furan-7-carboxylic acid chloride is prepared by reacting the parent acid with thionyl chloride for 3 hours under reflux. Pharmaceutical compositions having antidiabetic activity for enteral or parenetral administration comprise a compound of Formula I or a physiologically compatible salt thereof together with a liquid or solid pharmaceutical diluent or carrier