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    • 5. 发明申请
    • PROCESS FOR THE PREPARATION AND PURIFICATION OF ETRAVIRINE AND INTERMEDIATES THEREOF
    • 肝素及其中间体的制备和纯化方法
    • US20110275812A1
    • 2011-11-10
    • US13131698
    • 2010-07-27
    • Irena KrizmanicJasna DoganMarina MarinkovicMaja Sepelj
    • Irena KrizmanicJasna DoganMarina MarinkovicMaja Sepelj
    • C07D239/48C07D239/34
    • C07D239/34A61K31/505C07D239/42C07D239/48
    • In one embodiment the present invention encompasses 4-(2,6-dichloropyrimidin-4-yloxy)-3,5-dimethylbenzonitrile (“ETHER”), 4-(4,6-dichloropyrimidin-2-yloxy)-3,5-dimethyl-benzonitrile (“ETHER C-2 isomer”), mixtures and salts thereof of. The present invention encompasses the use of ETHER and salts thereof to prepare Etravirine and Etravirine intermediates, and salts thereof. In another embodiment the present invention encompasses the use of ETHER and salts thereof to prepare debrometravirine (“DEBETV”) and salts thereof. In yet another embodiment the present invention encompasses the use of ETHER and salts thereof to prepare 4-(6-chloro-2-(4-cyanophenylamino)pyrimidin-4-yloxy)-3,5-dimethyl-benzonitrile (“ARCPBN”) and salts thereof. The compound, 4-(2,6-dichloropyrimidin-4-yloxy)-3,5-dimethylbenzonitrile “ETHER” of formula (A) wherein n is either 0 or 1 and HA is an acid.
    • 在一个实施方案中,本发明包括4-(2,6-二氯嘧啶-4-基氧基)-3,5-二甲基苄腈(“ETHER”),4-(4,6-二氯嘧啶-2-基氧基) 二甲基 - 苄腈(“ETHER C-2异构体”),其混合物和盐。 本发明包括ETHER及其盐在制备Etravirine和Etravirine中间体及其盐中的应用。 在另一个实施方案中,本发明包括使用ETHER及其盐来制备脱敏瑞拉林(“DEBETV”)及其盐。 在另一个实施方案中,本发明包括醚及其盐在制备4-(6-氯-2-(4-氰基苯基氨基)嘧啶-4-基氧基)-3,5-二甲基 - 苄腈(“ARCPBN”)中的用途, 及其盐。 化合物,式(A)的4-(2,6-二氯嘧啶-4-基氧基)-3,5-二甲基苄腈“ETHER”,其中n为0或1,HA为酸。