会员体验
专利管家(专利管理)
工作空间(专利管理)
风险监控(情报监控)
数据分析(专利分析)
侵权分析(诉讼无效)
联系我们
交流群
官方交流:
QQ群: 891211   
微信请扫码    >>>
现在联系顾问~
热词
    • 9. 发明公开
    • CONVENIENT PREPARATION OF N-SUBSTITUTED MORPHINAN-6-OLS FROM MORPHINAN-6-ONES
    • VEREINFACHTE HERSTELLUNG VON N-SUBSTITUIERTEN MORPHINAN-6-OLEN AUS MORPHANAN-6-ONEN
    • EP3063152A1
    • 2016-09-07
    • EP14858224.0
    • 2014-10-31
    • Mallinckrodt LLC
    • WANG, Peter X.JIANG, Tao
    • C07D489/02
    • C07D489/08
    • Described herein are one-pot methods for preparing N-alkyl morphinan-6-ols from morphinan-6-ones. In particular, the methods comprise contacting a morphinan-6-one with a boron-based reducing agent and either a carbonyl compound, an acylating agent, or an alkylating agent. Disclosed herein are one-pot methods wherein the NH group is treated with a carbonyl compound, such as an aldehyde or ketone, and a reducing agent, and wherein the 6-keto group is reduced to a 6-hydroxy group; one-pot methods wherein the NH group is treated with an alkylating agent and a base, thereby generating an N-alkyl group, and wherein the 6-keto group is reduced to a 6-hydroxy group by the addition of a reducing agent; and methods wherein the NH group is acylated with an acylating agent and a base, thereby generating an N-acyl group, and wherein the 6-keto group is reduced to a 6-hydroxy group by the addition of a reducing agent.
    • 本文描述的是从吗啡喃-6-酮制备6-羟基N-烷基吗啡喃-6-ols的方法,如下所示:其中变量R1,R2,R3,R10,R11,R14如本文所定义,其中 反应在使用硼基还原剂的一锅法中发生。