Process for the preparation of 8-(4-aminophenoxy)-4H-pyrido[2,3-b]pyrazin-3-one derivatives
申请人:CANCER RESEARCH TECHNOLOGY LIMITED
公开号:US10100053B2
公开(公告)日:2018-10-16
The present invention pertains generally to the field of organic chemical synthesis, and in particular to certain methods for the synthesis of 8-(4-aminophenyoxy)-4H-pyrido[2,3-b]pyrazin-3-one and related compounds (denoted herein as (3)) from 4-(4-aminophenyoxy)pyridine-2,3-diamine and related compounds (denoted herein as (1)), by reaction with glyoxylic acid (denoted herein as (2)). The compounds (3) are useful in the synthesis of known anti-cancer agents, such as 1-(5-tert-butyl-2-(4-methyl-phenyl)-pyrazol-3-yl)-3-[2-fluoro-4-[(3-oxo-4H-pyrido[2,3-b]pyrazin-8-yl)oxy]phenyl]urea.
本发明一般涉及有机化学合成领域,特别涉及从 4-(4-氨基苯氧基)吡啶-2,3-二胺及相关化合物(在此表示为(1))通过与乙醛酸(在此表示为(2))反应合成 8-(4-氨基苯氧基)-4H-吡啶并[2,3-b]吡嗪-3-酮及相关化合物(在此表示为(3))的某些方法。化合物 (3) 可用于合成已知的抗癌剂,如 1-(5-叔丁基-2-(4-甲基苯基)-吡唑-3-基)-3-[2-氟-4-[(3-氧代-4H-吡啶并[2,3-b]吡嗪-8-基)氧基]苯基]脲。