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公开(公告)号：US20090192310A1
公开(公告)日：2009-07-30
申请号：US12419050
申请日：2009-04-06
IPC分类号： C07D411/04
CPC分类号： C07D411/04
摘要： A novel process for preparing emtricitabine, and more particularly a process for preparing emtricitabine involving the formation and isolation of intermediate compounds in salified form, is described.
摘要翻译： 描述了一种制备恩曲他滨的新方法，更具体地涉及一种涉及以成盐形式形成和分离中间体化合物的恩曲他滨的制备方法。
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公开(公告)号：US20060189805A1
公开(公告)日：2006-08-24
申请号：US10550718
申请日：2004-03-19
IPC分类号： A61K31/513 , C07D409/02
CPC分类号： C07D411/04
摘要： A process is disclosed for the stereo-selective preparation of emtricitabine, which allows the desired product to be obtained in good yield and without the use of chromatographic techniques. The process for the production of emtricitabine of the formula (Ia) is characterized by the formation and isolation of intermediate compounds of formula (XIa) in salified form. Emtricitabine is a known antiviral drug.
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公开(公告)号：US07534885B2
公开(公告)日：2009-05-19
申请号：US10550718
申请日：2004-03-19
IPC分类号： C07D411/04 , A61K31/513 , A61K31/12
CPC分类号： C07D411/04
摘要： A process is disclosed for the stereo-selective preparation of emtricitabine, which allows the desired product to be obtained in good yield and without the use of chromatographic techniques. The process for the production of emtricitabine of the formula (Ia) is characterized by the formation and isolation of intermediate compounds of formula (XIa) in salified form. Emtricitabine is a known antiviral drug.
摘要翻译： 公开了用于立曲达因选择性制备恩曲他滨的方法，其允许以良好的产率获得所需的产物，而不使用色谱技术。 制备式（Ia）的恩曲他滨的方法的特征在于以成盐形式形成和分离式（XIa）的中间体化合物。 恩曲他滨是一种已知的抗病毒药物。
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公开(公告)号：US07939660B2
公开(公告)日：2011-05-10
申请号：US12419050
申请日：2009-04-06
IPC分类号： C07D411/04 , C07D327/04 , A61K31/513 , A61P31/12
CPC分类号： C07D411/04
摘要： A novel process for preparing emtricitabine, and more particularly a process for preparing emtricitabine involving the formation and isolation of intermediate compounds in salified form, is described.
摘要翻译： 描述了一种制备恩曲他滨的新方法，更具体地涉及一种涉及以成盐形式形成和分离中间体化合物的恩曲他滨的制备方法。
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5.发明申请Process for preparing (s)-tetrahydro-a-(1-methylethyl)-2-oxo-1(2h)-pyrimidineacetic acid 审中-公开制备四氢-α-（1-甲基乙基）-2-氧代-1（2h） - 嘧啶乙酸的方法公开(公告)号：US20050222184A1
公开(公告)日：2005-10-06
申请号：US10515964
申请日：2003-05-28
IPC分类号： C07B61/00 , C07D239/10 , A61K31/513 , C07D239/02
CPC分类号： C07D239/10
摘要： A process for preparing (S)-tetrahydro-a-(1-methylethyl)-2-oxo-1(2H)-pyrimidineacetic acid, an intermediate that is useful in the synthesis of HIV protease inhibitors such as, for example, those described in U.S. Pat. No. 5,914,332, is described. The process under consideration comprises the following steps:—L-valine is reacted with acrylonitrile;—the N-(2-cyanoethyl)-L-valine thus obtained is isolated and then reacted with an alkyl chloroformate;—the N-(2-cyanoethyl)-N-(alkoxycarbonyl)-L-valine thus obtained is hydro-genated in the presence of a hydrogenation catalyst, preferably rhodium;—the N-(3-aminopropyl)-N-(methoxycarbonyl)-L-valine thus obtained is cyclized to give the desired compound.
摘要翻译： 制备（S） - 四氢-α-（1-甲基乙基）-2-氧代-1（2H） - 嘧啶乙酸的方法，该中间体可用于合成HIV蛋白酶抑制剂，例如所述的那些 在美国Pat。 第5,914,332号。 所考虑的方法包括以下步骤：将-L-缬氨酸与丙烯腈反应;分离得到的N-（2-氰基乙基）-L-缬氨酸，然后与氯甲酸烷基酯反应; - N-（2-氰基乙基） 氰基乙基）-N-（烷氧基羰基）-L-缬氨酸在氢化催化剂，优选铑的存在下氢化;由此获得的N-（3-氨基丙基）-N-（甲氧基羰基）-L-缬氨酸 环化得到所需化合物。
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