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1.发明公开SELECTIVE ENZYMATIC ESTERIFICATION AND SOLVOLYSIS OF EPIMERIC VITAMIN D ANALOG AND SEPARATION OF THE EPIMERS 有权酶促选择性酯化和溶剂分解差向异构体维生素D类似物和差向异构体分离
公开(公告)号：EP1470220A2
公开(公告)日：2004-10-27
申请号：EP03729607.6
申请日：2003-01-09
IPC分类号： C12N9/20
CPC分类号： C12P7/18 , C12P41/004
摘要： Provided is a method of selectively enzymatically esterifying or selectively enzymatically solvolyzing epimers of analogs of vitamin D having a stereogenic center at C-24 that has a free or esterified OH group. The method can be used, for example, for separating mixed epimers of the vitamin D analog.
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公开(公告)号：EP1646612A1
公开(公告)日：2006-04-19
申请号：EP05739023.9
申请日：2005-04-21
发明人： SHAPIRO, Evgeny , YAHALOMI, Ronit , NIDDAM-HILDESHEIM, Valerie , STERIMBAUM, Greta , CHEN, Kobi
IPC分类号： C07D215/18
CPC分类号： C07D215/18
摘要： The present invention provides processes for preparing montelukast.
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公开(公告)号：EP1904448B1
公开(公告)日：2011-02-02
申请号：EP06786369.6
申请日：2006-07-05
发明人： STERIMBAUM, Greta , SHAPIRO, Evgeny , CHEN, Kobi
IPC分类号： C07D215/18
CPC分类号： C07D215/18
摘要： The present invention provides methods of purifying montelukast, a new isolated impurity of montelukast of formula I, method for its isolation, and method of using montelukast impurity as a reference marker and a reference standard.
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4.发明授权SELECTIVE ENZYMATIC ESTERIFICATION AND SOLVOLYSIS OF EPIMERIC VITAMIN D ANALOG AND SEPARATION OF THE EPIMERS 有权酶促选择性酯化和溶剂分解差向异构体维生素D类似物和差向异构体分离
公开(公告)号：EP1470220B1
公开(公告)日：2011-10-05
申请号：EP03729607.6
申请日：2003-01-09
IPC分类号： C12P41/00
CPC分类号： C12P7/18 , C12P41/004
摘要： Provided is a method of selectively enzymatically esterifying or selectively enzymatically solvolyzing epimers of analogs of vitamin D having a stereogenic center at C-24 that has a free or esterified OH group. The method can be used, for example, for separating mixed epimers of the vitamin D analog.
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公开(公告)号：EP1646612B1
公开(公告)日：2009-07-01
申请号：EP05739023.9
申请日：2005-04-21
发明人： SHAPIRO, Evgeny , YAHALOMI, Ronit , NIDDAM-HILDESHEIM, Valerie , STERIMBAUM, Greta , CHEN, Kobi
IPC分类号： C07D215/18
CPC分类号： C07D215/18
摘要： The present invention provides processes for preparing montelukast.
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公开(公告)号：EP2046790A2
公开(公告)日：2009-04-15
申请号：EP08726227.5
申请日：2008-02-27
发明人： DOLITZKY, Ben-zion , SHAPIRO, Evgeny , INI, Santiago , SHMUELY, Yaron , LANCRY, Eli , PILARSKY, Gideon
IPC分类号： C07D471/04
CPC分类号： C07D213/73 , C07D471/04
摘要： The present invention provides processes of preparing 3-(2-chloroethyl)- 6,7,8,9-tetrahydro-9-hydroxy-2-methyl-4H-pyrrido[ 1,2-a]- pyrimidin-4-one (CMHTP) useful as intermediates for the preparation of paliperidone, wherein the processes use 3-(2-chloroethyl)-2-methyl-9-benzyloxy-4H-pyrido[ 1,2-a]pyrimidine-4- one (CMBP) and/or 3-(2-chloroethyl)-2-methyl-9-hydoxy-4H-pyrido[l,2- a]pyrimidine-4-one (CMHP) having phosphorus at least partially removed as the intermediate.
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公开(公告)号：EP1904448A1
公开(公告)日：2008-04-02
申请号：EP06786369.6
申请日：2006-07-05
发明人： STERIMBAUM, Greta , SHAPIRO, Evgeny , CHEN, Kobi
IPC分类号： C07D215/18
CPC分类号： C07D215/18
摘要： The present invention provides methods of purifying montelukast, a new isolated impurity of montelukast of formula I, method for its isolation, and method of using montelukast impurity as a reference marker and a reference standard.
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8.发明公开PROCESS FOR PREPARING NATEGLINIDE AND INTERMEDIATES THEREOF 审中-公开VERFAHREN ZUR HERSTELLUNG VON NATEGLINID SOWIE ZWISCHENPRODUKTE
公开(公告)号：EP1487782A1
公开(公告)日：2004-12-22
申请号：EP03763310.4
申请日：2003-07-03
IPC分类号： C07C231/02 , C07C231/24 , C07C233/63 , C07C51/60 , C07C61/08
CPC分类号： C07C231/24 , A61K31/16 , A61K31/198 , C07B2200/13 , C07C51/60 , C07C231/02 , C07C2601/14 , C07C61/08 , C07C233/63
摘要： Provided is a process for preparation of an intermediate in the synthesis of nateglinide. Trans-4-isopropylcyclohexane acid chloride is formed by reacting 4-isopropylcyclohexanecarboxyl acid with thionyl chloride in the presence of an effective amount of an organic amide. Also provided are processes for preparation of nateglinide by acylation of a suitable salt of D-phenylalanine with trans-4-isopropylcyclohexane acid chloride in both a single and a two phase system, and in water free of a co-solvent.
摘要翻译： 提供了那格列奈合成中的中间体的方法。 反式-4-异丙基环己烷酰氯通过4-异丙基环己烷羧酸与亚硫酰氯在有效量的有机酰胺存在下反应形成。 还提供了通过在单一和两相系统中以及不含共溶剂的水中酰化合成D-对苯丙氨酸盐与反式-4-异丙基环己烷酰氯制备那格列奈的方法。
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