-
1.发明公开LIPASE CATALYZED DYNAMIC RESOLUTION OF ISOXAZOLINE THIOESTERS TO ISOXAZOLINE CARBOXYLIC ACIDS 失效异恶唑啉硫TO异恶唑啉碳氢酸脂肪酶催化动力学分离
公开(公告)号：EP0971906A1
公开(公告)日：2000-01-19
申请号：EP98915165.9
申请日：1998-03-26
发明人： ZHANG, Lin-Hua , ANZALONE, Luigi , PESTI, Jaan, A. , YIN, Jianguo
IPC分类号： C07D261/04 , C12P41/00
CPC分类号： C12P17/14 , C07D261/04 , C12P41/005
摘要： The present invention relates generally to a novel lipase catalyzed transesterification for preparation of substituted isoxazolin-5-yl acetic acid in high optical purity from a stereoisomeric mixture of an esterified substituted isoxazolin-5-yl acetate. The products are useful in the synthesis of compounds for pharmaceuticals, especially the treatment of thrombolytic disorders, and agricultural products.
-
2.发明公开NOVEL ASYMMETRIC SYNTHESIS OF R-$g(a)-PROPYL-PIPERONYL AMINE AND ITS ANALOGS 失效R-ALFA丙基胡椒胺及其类似物的不对称合成
公开(公告)号：EP0888329A1
公开(公告)日：1999-01-07
申请号：EP97914876.0
申请日：1997-03-17
CPC分类号： C07D317/58
摘要： Processes for the preparation of R-α-propyl-piperonyl amine and its analogs, such compounds being useful intermediates in the preparation of elastase inhibitors, and intermediates useful for making R-α-propyl-piperonyl amine are described.
-
3.发明公开PREPARATION OF ASYMMETRIC CYCLIC UREAS THROUGH A MONOACYLATED DIAMINE INTERMEDIATE 审中-公开不对称环脲在单酰基DIAMIN中间体生产
公开(公告)号：EP1025092A2
公开(公告)日：2000-08-09
申请号：EP98952107.5
申请日：1998-10-06
发明人： STONE, Benjamin, R., P. , ANZALONE, Luigi , FORTUNAK, Joseph, M. , HARRIS, Gregory, D. , VALVIS, Ioannis, I. , WALTERMIRE, Robert, E.
IPC分类号： C07D243/00
CPC分类号： C07D491/04 , C07D243/04 , C07D317/14
摘要： The present invention concerns an improved process for the preparation of asymmetric cyclic ureas as well as intermediates in the preparation of asymmetric cyclic ureas of formula (VI): wherein: R7 is selected from the following: C¿1?-C8 alkyl substituted with 0-3 R?11; C¿2-C8 alkenyl substituted with 0-3 R11; C2-C8 alkynyl substituted with 0-3 R11; and a C¿3?-C14 carbocyclic ring system substituted with 0-3 R?11; R10 is C1-C10¿ alkyl, benzyl, naphthylmethyl, 3,4-methylenedioxybenzyl, or C¿1?-C4 alkyl substituted with phenyl wherein said phenyl is substituted with 0-3 R?10a¿; G taken together along with the oxygen atoms to which G is attached forms a group selected from: -O-C(-CH¿2?CH2CH2CH2CH2-)-O-, -O-C(CH2CH3)2-O-, -O-C(CH3)(CH2CH3)-O-, -O-C(CH2CH2CH2CH3)2-O-, -O-C(CH3)(CH2CH(CH3)CH3)-O-, -O-CH(phenyl)-O-, OCH2O-, -OC(CH3)2O- and -OC(OCH3)(CH2CH2CH3)O-. In the process, a diamine of formula (I-a) is selectively monoacylated to give an asymmetric monoacylated diamine which can be converted into asymmetric intermediates. The asymmetric intermediates can be further alkylated, cyclized, and/or modified to give compounds which are useful as HIV protease inhibitors for the treatment of HIV infection. The invention allows for scalable preparation of a wide variety of asymmetrical cyclic ureas.
-
-
搜索结果
3 条记录 (耗时 0.008 秒)
