发明名称 Process for the preparation of 14-hydroxymorphinan derivatives
摘要 To prepare N-substituted 3-substituted 14-hydroxymorphinans of the formula <IMAGE> in which R<2> is lower alkyl and R is cyclobutylmethyl or cyclopropylmethyl, a compound of the formula V is reduced with borane in an inert organic solvent. The resulting boron complex of the compound of the formula VII is treated with an acid. To prepare compounds of the formula L in which R<2> is hydrogen, treatment is carried out in another process step with NaSC2H5, hydrobromic acid, boron tribromide or pyridine hydrochloride. The resulting compounds have narcotic/analgesic properties without generating dependency. <IMAGE>
申请公布号 CH629783(A5) 申请公布日期 1982.05.14
申请号 CH19770003580 申请日期 1977.03.22
申请人 BRISTOL-MYERS CO. 发明人 IVO MONKOVIC;CAROL BACHAND;HENRY WONG;GARY LIM
分类号 A61K31/435;A61P25/04;C07D217/20;C07D217/24;C07D221/28;(IPC1-7):C07D221/28 主分类号 A61K31/435
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