-
公开(公告)号:US20050148796A1
公开(公告)日:2005-07-07
申请号:US11068287
申请日:2005-02-28
申请人: Sonja MacKey , Michael Matison , Haifeng Wu , Michael Goble , Moses McMillan , Vikram Kalthod
发明人: Sonja MacKey , Michael Matison , Haifeng Wu , Michael Goble , Moses McMillan , Vikram Kalthod
IPC分类号: C07C211/15 , C07C303/40 , C07C311/08 , C07D307/20 , C07D307/33 , C07C311/13
CPC分类号: C07D307/33 , C07C211/15 , C07C303/40 , C07C311/08 , C07D307/20
摘要: A process for preparing (S)-(−)-N-[4-[4-[ethyl(6-fluoro-6-methylheptyl)amino]-1-hydroxylphenyl]methanesulfonamide hemifumarate salt, which comprises reacting N-[4-[(2S)-tetrahydro-5-hydroxy-2-furanyl]phenyl]methanesulfonamide(IIa) with fluoroamine (III) in the presence of triacetoxyborohydride and ethyl acetate to provide [4-[-4-[ethyl(6-fluoro-6-methylheptyl)amino]-1-hydroxylphenyl]methanesulfonamide(I) and then converting I into the hemifumarate salt Ia. A process for preparing IIa is also claimed as well as intermediates IIa-IId.
摘要翻译: 制备(S) - ( - ) - N- [4- [4- [乙基(6-氟-6-甲基庚基)氨基] -1-羟基苯基]甲磺酰胺半富马酸盐的方法,其包括使N- [4- [(2S) - 四氢-5-羟基-2-呋喃基]苯基]甲磺酰胺(IIa)与氟代胺(III)在三乙酰氧基硼氢化钠和乙酸乙酯存在下反应,得到[4- [4- 6-甲基庚基)氨基] -1-羟基苯基]甲磺酰胺(I),然后将I转化成半富马酸盐Ia。 还要求制备IIa的方法以及中间体IIa-IId。