AG-12286

4-[[4-氨基-5-(2,6-二氟苯甲酰基)-1,3-噻唑-2-基]氨基]苯磺酰胺Chemical Name: 4-[4-Amino-5-(2,6-difluorobenzoyl)thiazol-2-ylamino]benzenesulfonamide
CAS No. 223784-75-6
项目整合开发状态: Biological Testing
项目研究机构: Agouron (Originator)
合成路线: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: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.