| 摘要 |
A process for the preparation of substituted 5-hydroxy-2,3,4,5,6,7-hexahydrothiazolo[3,2-a]pyridines is characterized in that thiolates (V) are prepared by the condensation of aldehydes (II) with cyanoacetamide (III) and ketones (IV) in the presence of piperidine. Further short-time treatment of the thiolates with methyl ester of monochloroacetic acid (VI) in boiling ethanol is carried out. Stable substituted 5-hydroxy-2,3,4,5,6,7-hexahydrothiazolo[3,2-a]pyridines (I) are prepared. The ultimate yield is 54-88%. |
