Synthesis of arylsulphonylaminopyrimidine - derivatives which reduce level of sugar in blood

摘要

Synthesis of arylsulphonylaminopyrimidine derivatives which reduce level of sugar in blood. Cpds. of formula (I):- (where A = alkyl, cycloalkyl, aryl or aralkyl opt. with halogen or 1-3C alkyl or alkoxy substituents; X = alkyl; R1 = hydrocarbon or o-hydrocarbon or thioalkyl; R2 = H or lower alkyl; r1 and R2 together may form a 3-5 membered methylene ring) and their physiologically acceptable salts may be prepared from suitable aryl sulphonyl chloride and 2-amino-pyrimidine. If the sulphenyl or sulphinyl chloride is used the product requires oxidation; or aryl sulphonyl guanidine and ZCOCHR1COZ' where Z, Z' = H or alkoxy or Z' = R2. The hydroxyl groups in the product are replaced by halogens, and reductive dehalogenation gives desired product, or aryl-sulphonamide and pyrimidine substituted at position 2 with a reactive ester or lower trialkylammonium group.