E047/1

1-(2-丁基-1-苯并呋喃-3-基)-1-[5-[2-(二乙胺基)乙氧基]-2-噻嗯基]甲酮盐酸Chemical Name: 1-(2-Butyl-1-benzofuran-3-yl)-1-[5-[2-(diethylamino)ethoxy]-2-thienyl]methanone hydrochloride
CAS No. 128995-51-7, 128995-52-8 (free base)
项目整合开发状态: Phase II
项目研究机构: Ebewe (Originator)
合成路线:2-Butylbenzofuran (I) was acylated with 5-methoxythiophen-2-carbonyl chloride (II) in chloroform at 0 C to give the methanone compound (III).Ether cleavage of (III) was accomplished with borontribromide in chloroform to give the hydroxy compound (IV).Compound (IV) was treated with sodium methanolate and subsequently reacted with diethylaminoethylchloride in diethylcarbonate to give the alkylated product.This was treated with hydrochloric acid to yield crystaline E047/1.The final product was purified by two recrystallizations from an acetone/water mixture.