BMS-431051
Chemical Name: N-[5-[3-(4-Acetylpiperazin-1-ylcarbonyl)-5-aminobenzylsulfanyl]thiazol-2-yl]-4-(dimethylamino)benzamide
项目整合开发状态: Preclinical
项目研究机构: Bristol-Myers Squibb (Originator)
合成路线:The reductocondensation of 3-amino-5-(chloromethyl)benzoic acid methyl ester (I) with 2-aminothiazol-5-ylisothiocyanate (II) by means of NaBH4 gives the thioether (III),which is condensed with 4-(dimethylamino)benzoyl chloride (IV) by means of pyridine in dichloromethane to yield the amide (V).The hydrolysis of the ester group of (V) with NaOH in methanol affords the corresponding carboxylic acid (VI),which is finally condensed with 1-acetylpiperazine (VII) by means of WSC,HATU and DIEA in THF to provide the target piperazide.
📌 参考资料/链接：
参考文献标题:Selective Emt inhibitors: Discovery and SAR of 2-amino-[(5-thiomethyl)aryl]thiazoles
文献作者:Wityak,J.; Das,J.; Liu,C.; Lin,J.; Spergel,S.H.; Moquin,R.V.; Furch,J.A.; Doweiko,A.; Kanner,S.; Lin,T.-A.
参考来源:225th ACS Natl Meet (March 23 2003,New Orleans) 2003,Abst MEDI 257