Org-35030, Ro-60-0175

Chemical Name: 2(S)-1-(6-Chloro-5-fluoro-1H-indol-1-yl)-2-propanamine fumarate
项目整合开发状态: Preclinical
项目研究机构: Roche (Originator), Organon (Not Determined)
合成路线:Condensation of 6-chloro-5-fluoroindole (I) with (R)-2-methyloxyran (II) in the presence of NaH produced the chiral indolylpropanol (III).After conversion of (III) to the corresponding mesylate (IV) with methanesulfonyl chloride and triethylamine,displacement by NaN3 with inversion of the configuration afforded the (S)-azide (V).Subsequent hydrogenation of (V) using PtO2 yielded the title amine,which was isolated as the fumarate salt.