| 摘要 |
The present invention relates to new, efficient processes for the preparation of 5-(2-oxazolylalkylthio)-2-azacycloalkanoylaminothiazole compounds of formula Ior 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, CONR9R10, COR11 or COOR12;R9, R10, R11 and R12 are each independently hydrogen, alkyl or aryl;m equals 0 to 5; andn 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.
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