CN Patent

CN103992262B — 塞瑞替尼及其中间体的制备方法

Assigned to SCI GENERAL MATERIAL & CHEMICAL Inc. · Expires 2015-11-11 · 11y expired

What this patent protects

本发明揭示了一种可用于制备塞瑞替尼(Ceritinib)的中间体2-异丙氧基-5-甲基-4-(哌啶-4-基)卤代苯(I)及其制备方法,其制备包括如下步骤:以4-(5-异丙氧基-2-甲基-4-硝基苯基)吡啶(II)为原料,经催化氢化反应得到2-异丙氧基-5-甲基-4-(哌啶-4-基)苯胺(III);化合物(III)经桑德迈尔反应得到所述2-异丙氧基-5-甲基-4-(哌啶-4-基)卤代苯(I)。本发明还揭示了一种塞瑞替尼的制备方法,以2-异丙氧基-5-甲基-4-(哌啶-4-基)卤代苯(I)为原料,依次经取代、还原和取代反应制得塞瑞替尼(VIII),该制备方法…

USPTO Abstract

本发明揭示了一种可用于制备塞瑞替尼(Ceritinib)的中间体2-异丙氧基-5-甲基-4-(哌啶-4-基)卤代苯(I)及其制备方法,其制备包括如下步骤:以4-(5-异丙氧基-2-甲基-4-硝基苯基)吡啶(II)为原料,经催化氢化反应得到2-异丙氧基-5-甲基-4-(哌啶-4-基)苯胺(III);化合物(III)经桑德迈尔反应得到所述2-异丙氧基-5-甲基-4-(哌啶-4-基)卤代苯(I)。本发明还揭示了一种塞瑞替尼的制备方法,以2-异丙氧基-5-甲基-4-(哌啶-4-基)卤代苯(I)为原料,依次经取代、还原和取代反应制得塞瑞替尼(VIII),该制备方法工艺简洁、条件温和且副反应少,适合工业化放大。

Drugs covered by this patent

Patent Metadata

Patent number
CN103992262B
Jurisdiction
CN
Classification
Expires
2015-11-11
Drug substance claim
No
Drug product claim
No
Assignee
SCI GENERAL MATERIAL & CHEMICAL Inc.
Source
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