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公开(公告)号：EP1274704B1
公开(公告)日：2004-01-14
申请号：EP01917385.5
申请日：2001-04-10
IPC分类号： C07D405/04 , A61K31/505 , A61P31/12
CPC分类号： C07H19/06
摘要： The present invention relates to a process for preparing 5'-acetylstavudine, an intermediate which is useful in the preparation of 2',3'-didehydro-3'-deoxythymidine, an active principle with antiviral action which is commonly known as stavudine (D4T).
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公开(公告)号：EP1608644B1
公开(公告)日：2006-11-02
申请号：EP04721969.6
申请日：2004-03-19
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 characterized by the formation and isolation of intermediate compounds in salified form, is described.
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公开(公告)号：EP1678192A1
公开(公告)日：2006-07-12
申请号：EP04791727.3
申请日：2004-10-21
摘要： A process is described for the preparation of doxifluridine of formula (I) at high yields and with reduced formation of impurities, which comprises the reaction of coupling of a compound of formula (III) with a compound of formula (IV), as defined in the description, in the presence of a Lewis acid and in an inert organic solvent, characterized in that said Lewis acid is added at a temperature below 0°C.
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公开(公告)号：EP1608644A1
公开(公告)日：2005-12-28
申请号：EP04721969.6
申请日：2004-03-19
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 characterized by the formation and isolation of intermediate compounds in salified form, is described.
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5.发明公开
公开(公告)号：EP1554266A1
公开(公告)日：2005-07-20
申请号：EP03808838.1
申请日：2003-10-13
IPC分类号： C07D333/08 , C07D333/16
CPC分类号： C07D333/22 , C07D333/08 , C07D333/16
摘要： The present invention relates to a process for preparing 2,5-disubstituted 3-alkyl-thiophenes and more particularly to a process for preparing them that comprises an acylation reaction in position 5 of 2-substituted 3-alkylthiophenes. This process does not need reagents which are difficult to handle and does not need anhydrous conditions or inert atmosphere. The resulting product is obtained in high purity.
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6.发明公开PROCESS FOR PREPARING 2',3'-DIDEHYDRO-2',3'-DIDEOXYNUCLEOSIDES AND 2',3'-DIDEOXYNUCLEOSIDES 有权方法肺Hersel 2 '3'-脱氢-2' ，3'-二脱氧核苷和2'，3'-二脱氧核苷
公开(公告)号：EP1654270A1
公开(公告)日：2006-05-10
申请号：EP04744169.6
申请日：2004-07-29
摘要： A process for preparing 2',3'-didehydro-2',3'-dideoxynucleosides and 2',3'-dideoxynucleosides is described, which comprises the reductive elimination reaction of a compound of formula (I) in which X, Y, P' and B have the meanings given in the description, by reaction with zinc metal and a suitable activating agent, characterized in that the divalent zinc is removed by precipitation, from an organic phase, of the corresponding zinc sulfide, by adding a solution of a mineral sulfide to the said organic phase.
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7.发明授权
公开(公告)号：EP1554266B1
公开(公告)日：2006-03-22
申请号：EP03808838.1
申请日：2003-10-13
IPC分类号： C07D333/08 , C07D333/16
CPC分类号： C07D333/22 , C07D333/08 , C07D333/16
摘要： The present invention relates to a process for preparing 2,5-disubstituted 3-alkyl-thiophenes and more particularly to a process for preparing them that comprises an acylation reaction in position 5 of 2-substituted 3-alkylthiophenes. This process does not need reagents which are difficult to handle and does not need anhydrous conditions or inert atmosphere. The resulting product is obtained in high purity.
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8.发明公开PROCESS FOR PREPARING (S)-TETRAHYDRO-A-(1-METHYLETHYL)-2-OXO-1(2H)- PYRIMIDINEACETIC ACID 审中-公开制备（S） - 四氢-A-（1-甲基乙基）-2-氧-1（2H） - 嘧啶乙酸的方法
公开(公告)号：EP1513819A1
公开(公告)日：2005-03-16
申请号：EP03727812.4
申请日：2003-05-28
IPC分类号： C07D239/10
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 US-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） - 嘧啶乙酸的一种方法，一种可用于合成HIV蛋白酶抑制剂的中间体，例如描述于 描述的方法包括以下步骤： - 使L-缬氨酸与丙烯腈反应; - 分离由此获得的N-（2-氰乙基）-L-缬氨酸，然后与 烷基氯甲酸酯; - 由此获得的N-（2-氰乙基）-N-（烷氧羰基）-L-缬氨酸在加氢催化剂，优选铑存在下加氢; --N-（3-氨丙基）-N - （甲氧羰基）-L-缬氨酸环化得到所需化合物。
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9.发明公开PROCESS FOR THE PREPARATION OF PROTECTED 1-(1-AMINOALKYL)-OXIRANES 审中-公开制造方法PROTECTED 1-（1-氨基烷基）-OXIRANEN
公开(公告)号：EP1339667A1
公开(公告)日：2003-09-03
申请号：EP01970067.3
申请日：2001-09-27
IPC分类号： C07C229/10 , C07C229/14 , C07D301/02
CPC分类号： C07C229/36 , C07D301/02 , C07D303/36 , Y02P20/55
摘要： A method is described for the preparation of a compound of formula (formula see on enclosed paper version) where R is a protective group of the amino groups of the amino acids; R' is a C1-C10 alkyl radical, an aryl, an aralkyl or a group ArX(CH2)m; where Ar is an aryl, X = O, S, NR'; R' is a C1-C5 alkyl or aryl radical and m is an integer between 0 and 5; in which (a) the carboxyl group of a compound of formula (formula see on enclosed paper version) is activated by treatment with a group that is an activator of carboxyl groups; (b) the compound thus activated is made to condense with a trimethylsulphoxonium or tri-methylsulphonium ylide; (c) the keto-ylide thus obtained is reduced by reaction with a ketone-reducing agent; (d) the compound thus obtained is then cyclized to give the compound of formula IV by reaction with a base.
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公开(公告)号：EP1274704A1
公开(公告)日：2003-01-15
申请号：EP01917385.5
申请日：2001-04-10
IPC分类号： C07D405/04 , A61K31/505 , A61P31/12
CPC分类号： C07H19/06
摘要： The present invention relates to a process for preparing 5'-acetylstavudine, an intermediate which is useful in the preparation of 2',3'-didehydro-3'-deoxythymidine, an active principle with antiviral action which is commonly known as stavudine (D4T).
摘要翻译： 本发明涉及一种制备5'-乙酰司他丁的方法，该中间体用于制备2'，3'-二脱氢-3'-脱氧胸苷（一种通常称为司他夫定的具有抗病毒作用的活性成分）（D4T ）。
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