【药物名称】AG-12286
化学结构式(Chemical Structure):
参考文献No.39234
标题:4-Aminothiazole derivs., their preparation and their use as inhibitors of cyclin-dependent kinases
作者:Yang, Y.; Xiao, W.; Chu, S.S.; Li, L.; Chong, W.K.M.; Duvadie, R.R. (Agouron Pharmaceuticals, Inc.)
来源:WO 9921845
合成路线图解说明:

The bromination of 2',6'-difluoroacetophenone (I) using CuBr2 afforded bromoketone (II). Addition of cyanamide to 4-isothiocyanato-benzenesulfonamide (III) in the presence of potassium tert-butoxide generated the intermediate N-cyano isothiourea (IV). Subsequent condensation of (IV) with bromoketone (II) produced the target thiazole derivative.

合成路线图解说明:

Treatment of 1-(4-aminophenyl)-4-methylpiperazine (I) with thiophosgene and Na2CO3 afforded isothiocyanate (II). Subsequent condensation of (II) with cyanamide in the presence of potassium tert-butoxide, followed by reaction of the resulting intermediate (IV) with 2-chloro-2',6'-difluoroacetophenone (V) produced the title aminothiazole.

参考文献No.546387
标题:Novel ATP-site cyclin-dependent kinase (CDK) inhibitors: Selective CDK inhibitors
作者:Li, L.; Chong, W.K.M.; Duvadie, R.K.; et al.
来源:218th ACS Natl Meet (Aug 22 1999, New Orleans) 1999,Abst MEDI 214
合成路线图解说明:

The bromination of 2',6'-difluoroacetophenone (I) using CuBr2 afforded bromoketone (II). Addition of cyanamide to 4-isothiocyanato-benzenesulfonamide (III) in the presence of potassium tert-butoxide generated the intermediate N-cyano isothiourea (IV). Subsequent condensation of (IV) with bromoketone (II) produced the target thiazole derivative.

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