新产品编号:843715

Chemical Name: 4-(4-Bromo-3-thienylmethyl)-1H-imidazole fumarate
CAS No. 334917-95-2, 334917-94-1 (free base)
项目整合开发状态: Preclinical
项目研究机构: Johnson & Johnson (Originator)
合成路线:The reaction of 4-bromothiophene-3-carboxylic acid with SOCl2 gives the corresponding acyl chloride (II),which is condensed with N,O-dimethylhydroxylamine (III) to yield the amide (IV).The Grignard condensation of (IV) with 4-imidazolylmagnesium bromide (V) affords the methanone (VI),which is reduced with NaBH4 to the corresponding carbinol (VII).Finally,this alcohol is reduced and deprotected with BH3/Me2S in dichloromethane/THF.
📌 参考资料/链接:
参考文献标题:alpha2 Adrenoceptor agonists as potential analgesic agents.3.Imidazolylmethylthiophenes
文献作者:Boyd,R.E.; Press,J.B.; Rasmussen,C.P.; Raffa,R.B.; Codd,E.E.; Connelly,C.D.; Li,Q.S.; Martinez,R.P.; Lewis,M.A.; Almond,H.R.; Reitz,A.B.
参考来源:J Med Chem 2001,44(6),863