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
    • 95. 发明授权
    • Process for preparation of 1-[9H-carbazol-4-yloxy]-3-[{2-(2-(-methoxy)phenoxy)-ethyl}-amino]-propan-2-ol
    • 制备1- [9H-咔唑-4-基氧基] -3 - [{2-(2 - ( - 甲氧基)苯氧基) - 乙基} - 氨基] - 丙-2-醇
    • US07482471B2
    • 2009-01-27
    • US10553957
    • 2004-03-04
    • Vijay Chhangamal ChhabadaRajeev Budhdev RehaniRajamannar Thennati
    • Vijay Chhangamal ChhabadaRajeev Budhdev RehaniRajamannar Thennati
    • C07D209/82
    • C07D405/12C07D209/88
    • The present invention provides a process for preparation of 1-[9H-carbazol-4-yloxy]-3-[{2-(2-(methoxy)phenoxy)-ethyl}-amino]-propan-2-ol,a compound of formula 1 in racemic form or in the form of optically active R or S enantiomer or its pharmaceutically acceptable salt, comprising, reacting 4-(oxiranylmethoxy)-9H-carbazole, a compound of formula (2) or the R or S enantiomer thereof with a compound of formula (5), wherein R1 is benzyl or substituted benzyl group, in an aprotic organic solvent in presence of a catalyst to obtain a compound of formula (6), or the R or S enantiomer thereof, wherein R1 is as defined above. The resultant compound of formula (6) is subjected to debenzylation reaction by catalytic hydrogenation to obtain the compound of formula (1), if desired converting the resultant compound of formula (1) to a pharmaceutically acceptable salt thereof.
    • 本发明提供了制备1- [9H-咔唑-4-基氧基] -3 - [{2-(2-(甲氧基)苯氧基) - 乙基} - 氨基] - 丙-2-醇的方法, 包括使4-(环氧乙烷基甲氧基)-9H-咔唑,式(2)的化合物或其R或S对映异构体与式(2)的化合物反应,或者以旋光形式的R或S对映体或其药学上可接受的盐的形式, 与式(5)化合物反应,其中R1是苄基或取代的苄基,在非质子有机溶剂中,在催化剂存在下,得到式(6)化合物或其R或S对映异构体,其中R 1为 以上定义。 所得到的式(6)化合物通过催化氢化进行脱苄基化反应,得到式(1)化合物,如果需要将所得式(1)化合物转化为其药学上可接受的盐。