Process for preparing azacycloalkanoylaminothiazoles (LD 137e)

摘要

The present invention relates to new, efficient processes for the preparation of 5-(-2-oxyazolylalkylthio)-2-azacycloalkanoylaminothiazole compounds of formula I or a pharmaceutically acceptable salt thereof, wherein: R is alkyl, aryl or heteroaryl; R¹, R², R³, R⁴ and R⁵ are each independently hydrogen, alkyl, aryl or heteroaryl; R⁶ and R⁷ are each independently hydrogen, alkyl, aryl, heteroaryl, halogen, hydroxy or alkoxy; R⁸ is hydrogen, alkyl, aryl, heteroaryl, CONR⁹, R¹⁰, COR¹¹ or COOR¹²; R⁹, R¹⁰, R¹¹ and R¹² are each independently hydrogen, alkyl or aryl; m equals 0 to 5; and n equals 0 to 5, which are novel, potent inhibitors of cyclin dependent kinases (cdks). The present invention further concerns new key intermediate compounds, a quaternary ammonium salt of formula III' and a 2-oxazolylalkyl derivative of formula IX.