公开(公告)号：US5026873A

公开(公告)日：1991-06-25

申请号：US432028

申请日：1989-11-06

申请人： Neal G. Anderson ,  David A. Lust ,  Barbara J. Bennett ,  Alan F. Feldman ,  Robert E. Polomski

发明人： Neal G. Anderson ,  David A. Lust ,  Barbara J. Bennett ,  Alan F. Feldman ,  Robert E. Polomski

IPC分类号： C07D207/12 ,  A61K31/40 ,  A61P9/00 ,  C07D207/16 ,  C07D207/46 ,  C07D295/04

CPC分类号： C07D207/16

摘要： A process is disclosed for direct isolation of captopril from a substrate of the formula ##STR1## wherein R is lower alkyl or lower alkoxy. In this process, the substrate is first treated with an aqueous alkali metal hydroxide capable of forming a water-soluble salt of the substrate, wherein the alkali metal hydroxide has a concentration of 4M or greater. The substrate is then neutralized, preferably with a mineral acid. By this process, captopril may be directly crystallized from an aqueous solution, avoiding the prior art use of organic solvents and zinc treatment to reduce levels of sulfide and disulfide impurities, respectively. In an alternative embodiment, neutralization is carried out by use of a hydrogen-supplying ion exchange resin.

公开(公告)号：US4912230A

公开(公告)日：1990-03-27

申请号：US245086

申请日：1988-09-16

申请人： Neal G. Anderson ,  Christopher M. Cimarusti ,  David A. Lust

发明人： Neal G. Anderson ,  Christopher M. Cimarusti ,  David A. Lust

IPC分类号： C07D207/16

CPC分类号： C07D207/16

摘要： A process is provided for inverting a hydroxy function of a L-trans-hydroxy proline derivative to the corresponding L-cis-hydroxy proline sulfonate by a Modified Mitsunobu reaction process.

摘要翻译： 提供了通过改良Mitsunobu反应方法将L-反 - 羟基脯氨酸衍生物的羟基官能团转化为相应的L-顺 - 羟基脯氨酸磺酸盐的方法。

公开(公告)号：US06515170B1

公开(公告)日：2003-02-04

申请号：US09843226

申请日：2001-04-26

申请人： Ramesh N. Patel ,  Amit Banerjee ,  Venkata B. Nanduri ,  Steven L. Goldberg ,  Robert M. Johnston ,  Thomas P. Tully ,  Laszlo J. Szarka ,  Shankar Swaminathan ,  John J. Venit ,  Jerome L. Moniot ,  William J. Winter ,  Neal G. Anderson ,  David A. Lust ,  Gerard Crispino ,  Sushil K. Srivastava

发明人： Ramesh N. Patel ,  Amit Banerjee ,  Venkata B. Nanduri ,  Steven L. Goldberg ,  Robert M. Johnston ,  Thomas P. Tully ,  Laszlo J. Szarka ,  Shankar Swaminathan ,  John J. Venit ,  Jerome L. Moniot ,  William J. Winter ,  Neal G. Anderson ,  David A. Lust ,  Gerard Crispino ,  Sushil K. Srivastava

IPC分类号： C07C3200

CPC分类号： C07K5/06139 ,  A61K38/00 ,  C07K14/8103 ,  C12N9/1096

摘要： The present invention concerns an enzymatic oxidative deamination process of a dipeptide monomer to prepare an intermediate useful to prepare compounds having endopeptidase and angiotensin converting enzyme inhibition activity.

公开(公告)号：US06261810B1

公开(公告)日：2001-07-17

申请号：US09386588

申请日：1999-08-31

申请人： Ramesh N. Patel ,  Amit Banerjee ,  Venkata B. Nanduri ,  Laszlo J. Szarka ,  Shankar Swaminathan ,  John J. Venit ,  Jerome L. Moniot ,  David A. Lust ,  Sushil K. Srivastava

发明人： Ramesh N. Patel ,  Amit Banerjee ,  Venkata B. Nanduri ,  Laszlo J. Szarka ,  Shankar Swaminathan ,  John J. Venit ,  Jerome L. Moniot ,  David A. Lust ,  Sushil K. Srivastava

IPC分类号： C12P1718

CPC分类号： C07K5/06139 ,  A61K38/00 ,  C07K14/8103 ,  C12N9/1096

摘要： The present invention concerns an enzymatic oxidative deamination process of a dipeptide monomer to prepare an intermediate useful to prepare compounds having endopeptidase and angiotensin converting enzyme inhibition activity.

摘要翻译： 本发明涉及二肽单体的酶氧化脱氨过程，以制备可用于制备具有内肽酶和血管紧张素转化酶抑制活性的化合物的中间体。