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1.发明公开PREPARATION OF (S)-2-AMINO-6,6-DIMETHOXYHEXANOIC ACID METHYL ESTER VIA NOVEL DIOXOLANES 审中-公开（S）-2-氨基-6,6-二甲氧基己酸甲酯通过新型二氧化硅的制备
公开(公告)号：EP1121351A2
公开(公告)日：2001-08-08
申请号：EP99932163.1
申请日：1999-07-01
发明人： GODFREY, Jollie, D., Jr. , KRONENTHAL, David, R. , SCHWINDEN, Mark, D. , SRIVASTAVA, Sushil, K. , RAMIG, Keith , VENIT, John, J. , JASS, Paul, A. , RACHA, Saibaba , DILLON, John, L., Jr. , SOUNDARARAJAN, Nachimuthu , POWERS, Gerald, L. , KOTNIS, Atul, S.
IPC分类号： C07D317/26 , C07D317/28
CPC分类号： C07C229/22 , C07D317/30
摘要： The invention relates to the synthesis of 2-amino-6, 6-dimethoxy hexanoic acid, methyl ester and novel dioxalane intermediates thereof, from the reaction of glycinamide of formula I with dioxolane of formula II.
摘要翻译： 本发明涉及由式I的甘氨酰胺与式II的二氧戊环反应合成2-氨基-6,6-二甲氧基己酸，甲酯和其新二氧杂环戊烷中间体。
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公开(公告)号：EP1309535B1
公开(公告)日：2008-03-26
申请号：EP01961698.6
申请日：2001-07-20
IPC分类号： C07C45/61 , C07D301/00 , C07D301/24
CPC分类号： C07C269/06 , C07C221/00 , C07D303/36 , C07C271/18
摘要： The present invention relates to a process for the preparation of α' chloroketones, such as 4-phenyl-3-t-butyloxy-carbonylamino)-2-keto-1-chlorobutane by reacting certain aryl amino acid esters, e.g. N-(2-t-butoxycarbonyl)-L-phenylalanine-4-nitrophenyl ester, with a sulfur ylide compound to form the corresponding keto ylide compound which is then treated with a source of chloride and an organic acid.
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公开(公告)号：EP1089973B1
公开(公告)日：2005-11-09
申请号：EP99930402.5
申请日：1999-06-18
发明人： BISACCHI, Gregory , SLUSARCHYK, William, A. , TREUNER, Uwe , SUTTON, James, C. , ZAHLER, Robert , SEILER, Steven , KRONENTHAL, David, R. , RANDAZZO, Michael, E. , XU, Zhongmin , SHI, Zhongping , SCHWINDEN, Mark, D.
IPC分类号： C07D205/08 , C07D205/09 , C07D403/12 , C07D401/06 , C07D403/06 , A61K31/395
CPC分类号： C07D403/12 , C07D205/08
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4.发明公开PREPARATION OF [4S-(4ALPHA,7ALPHA,10ABETA)]-4-AMINO-OCTAHYDRO-5-OXO-7H-PYRIDO 2,1-B] 1,3]THIAZEPINE-7-CARBOXYLIC ACID, METHYL ESTER AND SALTS THEREOF VIA NOVEL DISULFIDES 审中-公开4S-制备（4-克（a）中，7-克（a）中，图10A-G（b）中）-4-氨基 - 八氢-5-氧代-7H-吡啶并2,1-B 1,3硫氮杂 -7-羧酸甲酯及其盐的VIA NEW DISULFIDE
公开(公告)号：EP1235792A1
公开(公告)日：2002-09-04
申请号：EP99974268.7
申请日：1999-07-29
发明人： MONIOT, Jerome, L. , RAMIG, Keith , JASS, Paul, A. , DILLON, John, L., Jr. , RACHA, Saibaba , SHRIVASTAVA, Sushil, K. , WINTER, William, J. , VENIT, John, J. , SWAMINATHAN, Shankar , SIMPSON, James , CHEN, Chien-Kuang , PACK, Shawn, K. , SCHWINDEN, Mark, D.
IPC分类号： C07C261/00 , C07C229/04 , C07C229/22 , C07D281/02
CPC分类号： Y02P20/55
摘要： N-protected-L-homocysteine disulfide of the formula (I) or an activated form thereof is reacted with (S)-2-amino-6,6-dimethoxyhexanoic acid, methyl ester to give the disulfide intermediate of the formula (II). The disulfide intermediate of formula (II) is reacted to cleave the disulfide bond and the resulting monomer is subjected to an acid catalyzed cyclization reaction to give the N-protected lactam of the formula (III). Removal of the N-protecting group gives [4S-(4α,7α,10aβ]-4-aminooctahydro-5-oxo-7H-pyrido[2,1-b][1,3]thiazepine-7-carboxylic acid, methyl ester which along with its salt is useful as an intermediate in the preparation of the dual inhibitor [4S- [4α(R*),7α,10aβ]]-octahydro-4-[(2-mercapto-1-oxo-3-phenylpropyl)amino]-5-oxo-7H-pyrido-[2,1-b][1,3]thiazepine-7-carboxylic acid.
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公开(公告)号：EP1309535A1
公开(公告)日：2003-05-14
申请号：EP01961698.6
申请日：2001-07-20
IPC分类号： C07C45/61 , C07D301/00 , C07D301/24
CPC分类号： C07C269/06 , C07C221/00 , C07D303/36 , C07C271/18
摘要： The present invention relates to a process for the preparation of α' chloroketones, such as 4-phenyl-3-t-butyloxy-carbonylamino)-2-keto-1-chlorobutane by reacting certain aryl amino acid esters, e.g. N-(2-t-butoxycarbonyl)-L-phenylalanine-4-nitrophenyl ester, with a sulfur ylide compound to form the corresponding keto ylide compound which is then treated with a source of chloride and an organic acid.
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公开(公告)号：EP1089973A1
公开(公告)日：2001-04-11
申请号：EP99930402.5
申请日：1999-06-18
发明人： BISACCHI, Gregory , SLUSARCHYK, William, A. , TREUNER, Uwe , SUTTON, James, C. , ZAHLER, Robert , SEILER, Steven , KRONENTHAL, David, R. , RANDAZZO, Michael, E. , XU, Zhongmin , SHI, Zhongping , SCHWINDEN, Mark, D.
IPC分类号： C07D205/08 , C07D205/09
CPC分类号： C07D403/12 , C07D205/08
摘要： Compounds of formulae (I), (II), (III).
摘要翻译： 式（I），（II），（III）的化合物。
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