公开(公告)号：US20060270012A1

公开(公告)日：2006-11-30

申请号：US11365275

申请日：2006-03-01

申请人： Nigel Bowers ,  Paul Skonezny ,  Gregory Stein ,  Thomas Franceschini ,  Shu-Jen Chiang ,  Wendy Anderson ,  Li You ,  Zizhou Xing

发明人： Nigel Bowers ,  Paul Skonezny ,  Gregory Stein ,  Thomas Franceschini ,  Shu-Jen Chiang ,  Wendy Anderson ,  Li You ,  Zizhou Xing

IPC分类号： C12P7/02

CPC分类号： C12R1/01 ,  C12P13/001

摘要： The present invention relates to a process for preparing (2R,3S)-1-halo-2-hydroxy-3-(protected)amino-4-substituted butane comprising contacting a mutagenized Rhodococcus erythropolis having ATCC deposit no. PTA-6648 with (3S)-1-halo-2-oxo-3-(protected)amino-4-substituted butane substrate. The present invention also relates to a process comprising mixing (2R,3S)-1-halo-2-hydroxy-3-(protected)amino-4-substituted butane with at least one base in the presence of at least one solvent to produce a reaction mixture containing (2R,3S)-1,2-epoxy-3-(protected)amino-4-substituted butane. The present invention further relates to a process comprising crystallizing the (2R,3S)-1,2-epoxy-3-(protected)amino-4-substituted butane out of the reaction mixture by concurrently adding water and the reaction mixture together. The present invention is also directed to a mutagenized Rhodococcus erythropolis having ATCC deposit no. PTA-6648.

公开(公告)号：US20050256019A1

公开(公告)日：2005-11-17

申请号：US11119552

申请日：2005-05-02

申请人： Ramesh Patel ,  Ronald Hanson ,  Iqbal Gill ,  David Brzozowski ,  Paul Skonezny ,  Michael Politino ,  Jason Chen ,  Francisco Moris-Varas ,  Brenda White

发明人： Ramesh Patel ,  Ronald Hanson ,  Iqbal Gill ,  David Brzozowski ,  Paul Skonezny ,  Michael Politino ,  Jason Chen ,  Francisco Moris-Varas ,  Brenda White

IPC分类号： C07D207/22 ,  C07D209/52 ,  C07K5/065 ,  C11D3/00 ,  C12P17/10

CPC分类号： C07D207/22 ,  C07D209/52 ,  C07K5/06078 ,  C12P13/04 ,  C12P17/10 ,  C12P17/12

摘要： An enzymatic ammonolysis process is provided for the preparation of intermediates used in preparing dipeptidyl peptidase IV inhibitors wherein the enzyme Candida antarctica lipase-B is used to catalyze the ammonolysis process.

摘要翻译： 提供酶促氨解方法用于制备用于制备二肽基肽酶IV抑制剂的中间体，其中使用南极假丝酵母脂肪酶-B来催化氨解过程。

公开(公告)号：US20050020685A1

公开(公告)日：2005-01-27

申请号：US10865422

申请日：2004-06-10

申请人： Paul Skonezny ,  Robert Stankavage ,  Gregory Stein

发明人： Paul Skonezny ,  Robert Stankavage ,  Gregory Stein

IPC分类号： C07D499/00 ,  A61K31/198 ,  C07C323/25

CPC分类号： C07D499/00

摘要： A process for recovering residual amounts of 6-APA, on the order of 10 g/L or less, from a predominantly aqueous liquor containing phenoxyacetic acid and less than about 2% organic solvents.

摘要翻译： 从含有苯氧基乙酸和小于约2％有机溶剂的主要含水液体中回收残留量为10g / L或更低的6-APA的方法。

公开(公告)号：US20050260712A1

公开(公告)日：2005-11-24

申请号：US11104015

申请日：2005-04-12

申请人： Michael Politino ,  Matthew Cadin ,  Paul Skonezny ,  Jason Chen

发明人： Michael Politino ,  Matthew Cadin ,  Paul Skonezny ,  Jason Chen

IPC分类号： C07H21/04 ,  C12N1/06 ,  C12N1/21 ,  C12N9/02 ,  C12N9/06 ,  C12N15/74 ,  C12P13/04 ,  C12P13/22 ,  C12P15/00 ,  C12P17/10 ,  C12P21/06

CPC分类号： C07D209/52 ,  C07H21/04 ,  C12N1/066 ,  C12N9/0008 ,  C12N9/0018 ,  C12P13/04 ,  C12P13/222 ,  C12P15/00 ,  C12P17/10 ,  C12Y102/02001

摘要： A process for production of cyclopropyl-fused pyrrolidine-based inhibitors of dipeptidyl peptidase IV is provided which employs a BOC-protected amine of the structure prepared by subjecting an acid of the structure to reduce amination by treating the acid with ammonium formate, nicotinamide adenine dinucleotide, dithiothreitol and partially purified phenylalanine dehydrogenase/formate dehydrogenase enzyme concentrate (PDH/FDH) and without isolating treating the resulting amine of the structure 2 with di-tert-butyl dicarbonate to form the BOC-protected amine.

摘要翻译： 提供了制备二肽基肽酶IV的环丙基稠合吡咯烷基抑制剂的方法，该方法采用BOC保护的胺，其结构是通过用甲酸铵，烟酰胺腺嘌呤二核苷酸处理酸来降低胺化而制备的结构 ，二硫苏糖醇和部分纯化的苯丙氨酸脱氢酶/甲酸脱氢酶浓缩物（PDH / FDH），并且不分离用二碳酸二叔丁酯处理所得结构2的胺以形成BOC保护的胺。

公开(公告)号：US20070207527A1

公开(公告)日：2007-09-06

申请号：US11736786

申请日：2007-04-18

申请人： Ramesh Patel ,  Ronald Hanson ,  Iqbal Gill ,  David Brzozowski ,  Paul Skonezny ,  Michael Politino ,  Jason Chen ,  Francisco Moris-Varas ,  Brenda White

发明人： Ramesh Patel ,  Ronald Hanson ,  Iqbal Gill ,  David Brzozowski ,  Paul Skonezny ,  Michael Politino ,  Jason Chen ,  Francisco Moris-Varas ,  Brenda White

IPC分类号： C12P13/24

CPC分类号： C07D207/22 ,  C07D209/52 ,  C07K5/06078 ,  C12P13/04 ,  C12P17/10 ,  C12P17/12

摘要： An enzymatic ammonolysis process is provided for the preparation of intermediates used in preparing dipeptidyl peptidase IV inhibitors wherein the enzyme Candida antarctica lipase-B is used to catalyze the ammonolysis process.

摘要翻译： 提供酶促氨解方法用于制备用于制备二肽基肽酶IV抑制剂的中间体，其中使用南极假丝酵母脂肪酶-B来催化氨解过程。