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,特别是涉及从
4-(4-氨基苯氧基)吡啶-2,3-二胺及相关化合物(以下简称为(1))与甘氧酸(以下简称为(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(以下简称为(3))的某些方法。这些化合物(3)在合成已知的抗癌药物中起到作用,例如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。