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
    • 4. 发明申请
    • PROCESS FOR THE PREPARATION OF BARICITINIB AND AN INTERMEDIATE THEREOF
    • 制备巴西替尼及其中间体的方法
    • WO2016088094A1
    • 2016-06-09
    • PCT/IB2015/059364
    • 2015-12-04
    • SUN PHARMACEUTICAL INDUSTRIES LIMITED
    • AZAD, Md Abul KalamPANDEY, GyanendraSINGH, KaptanPRASAD, Mohan
    • C07D487/04
    • C07D487/04C07D205/04C07D231/10
    • The present invention provides a process for the preparation of baricitinib and an intermediate thereof. The present invention provides a convenient, economical, and industrially advantageous two-step process for the preparation of [4-(IH-pyrazol-4-yl)-7Hpyrrolo[2,3-d] pyrimidin-7-yl]methyl pivalate of Formula (II). The process of the present invention involves the use of an alkali or alkaline earth metal hydroxide, carbonate, or bicarbonate as a base for reacting 4-chloro-7H-pyrrolo[2,3-d]pyrimidine of Formula (III) with chloromethyl pivalate of Formula (IV), and the use of an unprotected pyrazole borolane of Formula (VIII) for the conversion of (4-chloro-7H-pyrrolo[2,3-d] pynmidin-7- yl)methyl 2,2-dimethylpropanoate of Formula V into [4-(1 H-pyrazol-4-yl)-7Hpyrrolo[2,3-d]pyrimidin-7-yl]methyl pivalate of Formula (II). The process of the present invention provides [4-(1 H-pyrazol-4-yl)-7H-pyrrolo[2,3-d]pyrimidin-7-yl]methyl pivalate of Formula (I) in high yield.
    • 本发明提供了制备巴替西汀及其中间体的方法。 本发明提供了一种方便,经济和工业上有利的二步法,用于制备[4-(1H-吡唑-4-基)-7H-吡咯并[2,3-d]嘧啶-7-基]甲基新戊酸酯 式(II)。 本发明的方法涉及使用碱金属或碱土金属氢氧化物,碳酸盐或碳酸氢盐作为使式(III)的4-氯-7H-吡咯并[2,3-d]嘧啶与新戊酸氯甲酯反应的碱 的式(Ⅳ)化合物的用途,以及使用式(Ⅷ)的未保护的吡唑硼烷来转化(4-氯-7H-吡咯并[2,3-d] yn啶-7-基)甲基2,2-二甲基丙酸酯 式(II)的[4-(1H-吡唑-4-基)-7H-吡咯并[2,3-d]嘧啶-7-基]甲基。 本发明的方法以高产率提供式(I)的[4-(1H-吡唑-4-基)-7H-吡咯并[2,3-d]嘧啶-7-基]甲基。