Foropafant, SR-27417

福罗帕泛Chemical Name: 2-[N-[2-(Dimethylamino)ethyl]-N-(3-pyridylmethyl)amino]-4-(2,4,6-triisopropylphenyl)thiazole
CAS No. 136468-36-5
项目整合开发状态: Phase II
项目研究机构: Sanofi-Aventis (Originator)
合成路线:SR 27417 (N-(2-dimethylaminoethyl)-N-(3-pyridinylmethyl)[4-(2,4,6-triisopropylphenyl)thiazol-2-yl]amine difumarate) was prepared via a convergent route.Reductive amination of N,N-dimethylaminoethanamine (I) and pyridyl-3-carboxaldehyde (II) by sodium borohydride gave the amine (III).Eaction of pivaloyl chloride (IV) and potassium thiocyanate in anhydrous acetone provided the pivaloyl isothiocyanate (V),which was condensed in situ with the amine (III) to afford the protected thiourea (VI).Chlorhydric hydrolysis of (IV) gave the thiourea (VII) with the bromoketene (IX) in refluxing ethanol led to SR 27417.