Maleate salts of (e)-n-{ 4-[3-chloro-4-(2-pyridinylmethoxy)anilino]-3-cyano-7-ethoxy-6-quinolinyl} -4-(dimethylamino)-2-butenamide and crystalline forms thereof
LU QINGHONG,KU MANNCHING SHERRY,CHEW WARREN,CHEAL GLORIA K.,HADFIELD ANTHONY F.,MIRMEHRABI MAHMOUD
申请号：
NZ60034908
公开号：
NZ600349A
申请日:
2008.10.16
申请国别(地区):
NZ
年份:
2013
代理人:
摘要：
600349 Disclosed herein is a method of preparing (E)-N-{ 4-[3-chloro-4-(2-pyridinylmethoxy)anilino]-3-cyano-7-ethoxy-6-quinolinyl} -4-(dimethylamino)-2-butenamide as a maleate, monohydrate salt, comprising reacting the free base with maleic acid in a water-alcohol solution at a temperature in the range of between 50°C to 60°C Specifically, the crystalline form II characterised by X-ray diffraction peaks at the following angles (±0.20°) of 2theta in its X-ray diffraction pattern comprising 6.53, 8.43, 13.01, 15.17 and 16.76. The maleate salts are useful in treating cancers, particularly those affected by kinases of the epidermal growth factor receptor family.
