Ro-44-2104

Chemical Name: 4'-(N-Allyl-N-methylaminomethyl)-4-biphenylyl-4-bromophenyl ketone
CAS No. 140620-63-9, 140621-14-3 (HCl)
项目整合开发状态: Preclinical
项目研究机构: Roche (Originator)
合成路线:Grignard reagent (II) prepared from 1,4-dibromobenzene (I) was condensed with biphenylaldehyde (III) to afford alcohol (IV),which was oxidized to ketone (V) under Swern conditions with oxalyl chloride and DMSO at low temperature.Then,allylic bromination with N-bromosuccinimide (NBS) in the presence of azobisisobutyronitrile (AIBN) gave (VI).Finally,N-allyl-N-methylamine (VII) was alkylated with bromide (VI) to provide the tertiary amine.
📌 参考资料/链接:
参考文献标题:Use of phenylalkylamines for producing cholesterol lowering agents
文献作者:Aebi,J.; Guerry,P.; Jolidon,S.; Morand,O.(F.Hoffmann-La Roche AG)
参考来源:EP 0636367; JP 1995053479; US 5637771