公开(公告)号：US07074932B2

公开(公告)日：2006-07-11

申请号：US10431018

申请日：2003-05-07

申请人： Michael S. Allen ,  Ramiya H. Premchandran ,  Sou-Jen Chang ,  Stephen Condon ,  John A. DeMattei ,  Steven A. King ,  Lawrence Kolaczkowski ,  Sukumar Manna ,  Paul J. Nichols ,  Hemant H. Patel ,  Subhash R. Patel ,  Daniel J. Plata ,  Eric J. Stoner ,  Jien-Heh J. Tien ,  Steven J. Wittenberger

发明人： Michael S. Allen ,  Ramiya H. Premchandran ,  Sou-Jen Chang ,  Stephen Condon ,  John A. DeMattei ,  Steven A. King ,  Lawrence Kolaczkowski ,  Sukumar Manna ,  Paul J. Nichols ,  Hemant H. Patel ,  Subhash R. Patel ,  Daniel J. Plata ,  Eric J. Stoner ,  Jien-Heh J. Tien ,  Steven J. Wittenberger

IPC分类号： C07D215/16 ,  C07D215/18

CPC分类号： C07D215/14 ,  C07C68/06 ,  C07C69/96

摘要： The invention relates to a process for preparing quinoline-substituted carbonate and carbamate compounds, which are important intermediates in the synthesis of 6-O-substituted macrolide antibiotics. The process employs metal-catalyzed coupling reactions to provide a carbonate or carbamate of formula (I) or (II) or a substrate that can be reduced to obtain the same.

公开(公告)号：US06579986B2

公开(公告)日：2003-06-17

申请号：US10134777

申请日：2002-04-29

申请人： Michael S. Allen ,  Ramiya H. Premchandran ,  Sou-Jen Chang ,  Stephen Condon ,  John A. DeMattei ,  Steven A. King ,  Lawrence Kolaczkowski ,  Sukumar Manna ,  Paul J. Nichols ,  Hemant H. Patel ,  Subhash R. Patel ,  Daniel J. Plata ,  Eric J. Stoner ,  Jien-Heh J. Tien ,  Steven J. Wittenberger

发明人： Michael S. Allen ,  Ramiya H. Premchandran ,  Sou-Jen Chang ,  Stephen Condon ,  John A. DeMattei ,  Steven A. King ,  Lawrence Kolaczkowski ,  Sukumar Manna ,  Paul J. Nichols ,  Hemant H. Patel ,  Subhash R. Patel ,  Daniel J. Plata ,  Eric J. Stoner ,  Jien-Heh J. Tien ,  Steven J. Wittenberger

IPC分类号： C07D21536

CPC分类号： C07D215/14 ,  C07C68/06 ,  C07C69/96

摘要： The invention relates to a process for preparing quinoline-substituted carbonate and carbamate compounds, which are important intermediates in the synthesis of 6-O-substituted macrolide antibiotics. The process employs metal-catalyzed coupling reactions to provide a carbonate or carbamate of formula (I) or (II) or a substrate that can be reduced to obtain the same.

公开(公告)号：US5541328A

公开(公告)日：1996-07-30

申请号：US415385

申请日：1995-04-03

申请人： Timothy L. Stuk ,  Michael S. Allen ,  Anthony R. Haight ,  Francis A. Kerdesky ,  Denton C. Langridge ,  M. Robert Leanna ,  Linda M. Lijewski ,  Laura Melcher ,  Howard E. Morton ,  Daniel W. Norbeck ,  Daniel S. Reno ,  Timothy A. Robbins ,  Hing L. Sham ,  Thomas J. Sowin ,  Jien-Heh J. Tien ,  Chen Zhao ,  David Scarpetti

发明人： Timothy L. Stuk ,  Michael S. Allen ,  Anthony R. Haight ,  Francis A. Kerdesky ,  Denton C. Langridge ,  M. Robert Leanna ,  Linda M. Lijewski ,  Laura Melcher ,  Howard E. Morton ,  Daniel W. Norbeck ,  Daniel S. Reno ,  Timothy A. Robbins ,  Hing L. Sham ,  Thomas J. Sowin ,  Jien-Heh J. Tien ,  Chen Zhao ,  David Scarpetti

IPC分类号： C07C213/00 ,  C07C215/28 ,  C07C225/16 ,  C07C227/18 ,  C07C229/36 ,  C07C231/12 ,  C07C233/35 ,  C07C251/40 ,  C07C255/27 ,  C07C255/42 ,  C07C269/06 ,  C07C271/20 ,  C07D209/44 ,  C07D221/14 ,  C07C251/78 ,  C07C209/44 ,  C07C221/14

CPC分类号： C07D221/14 ,  C07C213/00 ,  C07C215/28 ,  C07C225/16 ,  C07C251/40 ,  C07C255/42 ,  C07C269/06 ,  C07C271/20 ,  C07D209/44 ,  C07B2200/07

摘要： A substantially pure compound of formula: ##STR1## wherein R.sub.6 and R.sub.7 are independently selected from ##STR2## wherein R.sub.a and R.sub.b are independently selected from hydrogen, loweralkyl and phenyl and R.sub.c, R.sub.d and R.sub.e are independently selected from hydrogen, loweralkyl, trifluoromethyl, alkoxy, halo and phenyl; and ##STR3## wherein the naphthyl ring is unsubstituted or substituted with one, two or three substitutents independently selected from loweralkyl, trifluoromethyl, alkoxy and halo; orR.sub.6 is as defined above and R.sub.7 is R.sub.7a OC(O)-- wherein R.sub.7a is loweralkyl; orR.sub.6 and R.sub.7 taken together with the nitrogen atom to which they are bonded are ##STR4## wherein R.sub.f, R.sub.g, R.sub.h and R.sub.l are independently selected from hydrogen, loweralkyl, alkoxy, halogen and trifluoromethyl; andR.sub.g is hydrogen, loweralkyl or benzyl; or an acid addition salt thereof.

摘要翻译： （I）其中R a和R b独立地选自氢，低级烷基和苯基，R c，R d和R 10独立地选自氢，低级烷基 ，三氟甲基，烷氧基，卤素和苯基; （ii）其中萘基环是未取代的或被一个，两个或三个独立地选自低级烷基，三氟甲基，烷氧基和卤素的取代基取代; 或R 6如上所定义，且R 7为R 7aa（O） - ，其中R 7a为低级烷基; 或者R 6和R 7与它们所键合的氮原子一起是其中R f，R g，R h和R 1独立地选自氢，低级烷基，烷氧基，卤素和三氟甲基; R g为氢，低级烷基或苄基; 或其酸加成盐。

公开(公告)号：US5543549A

公开(公告)日：1996-08-06

申请号：US415403

申请日：1995-04-03

申请人： Timothy L. Stuk ,  Michael S. Allen ,  Anthony R. Haight ,  Howard E. Morton ,  Daniel S. Reno ,  Hing L. Sham ,  Thomas J. Sowin ,  Jien-Heh J. Tien

发明人： Timothy L. Stuk ,  Michael S. Allen ,  Anthony R. Haight ,  Howard E. Morton ,  Daniel S. Reno ,  Hing L. Sham ,  Thomas J. Sowin ,  Jien-Heh J. Tien

IPC分类号： C07C213/00 ,  C07C215/28 ,  C07C225/16 ,  C07C227/18 ,  C07C229/36 ,  C07C231/12 ,  C07C233/35 ,  C07C251/40 ,  C07C255/27 ,  C07C255/42 ,  C07C269/06 ,  C07C271/20 ,  C07D209/44 ,  C07D221/14 ,  C07C255/00 ,  C07C233/00 ,  C07C261/00 ,  C07D209/04

CPC分类号： C07D221/14 ,  C07C213/00 ,  C07C215/28 ,  C07C225/16 ,  C07C251/40 ,  C07C255/42 ,  C07C269/06 ,  C07C271/20 ,  C07D209/44 ,  C07B2200/07

摘要： Intermediates and processes are disclosed which are useful for the preparation of a substantially pure compound of the formula: ##STR1## wherein R.sub.6 and R.sub.7 are each hydrogen or R.sub.6 and R.sub.7 are independently selected from ##STR2## wherein R.sub.a and R.sub.b are independently selected from hydrogen, loweralkyl and phenyl and R.sub.c, R.sub.d and R.sub.e are independently selected from hydrogen, loweralkyl, trifluoromethyl, alkoxy, halo and phenyl; and ##STR3## wherein the naphthyl ring is unsubstituted or substituted with one, two or three substitutents independently selected from loweralkyl, trifluoromethyl, alkoxy and halo; orR.sub.6 is as defined above and R.sub.7 is R.sub.7a OC(O)-- wherein R7a is loweralkyl or benzyl; orR.sub.6 and R.sub.7 taken together with the nitrogen atom to which they are bonded are ##STR4## wherein R.sub.f, R.sub.g, R.sub.h and R.sub.i are independently selected from hydrogen, loweralkyl, alkoxy, halogen and trifluoromethyl and R.sub.8 is hydrogen or --C(O)R" wherein R" is loweralkyl, alkoxy, benzyloxy or phenyl wherein the phenyl ring is unsubstituted or substituted with one, two or three substituents independently selected from loweralkyl, trifluoromethyl, alkoxy and halo; or an acid addition salt thereof.

摘要翻译： 公开了用于制备基本上纯的下式化合物的中间体和方法：其中R 6和R 7各自为氢或R 6和R 7独立地选自（ⅰ）其中R a和R b独立地为 选自氢，低级烷基和苯基，R c，R d和R e独立地选自氢，低级烷基，三氟甲基，烷氧基，卤素和苯基; （ii）其中萘基环是未取代的或被一个，两个或三个独立地选自低级烷基，三氟甲基，烷氧基和卤素的取代基取代; 或R 6如上所定义，R 7为R 7aa（O） - ，其中R 7a为低级烷基或苄基; 其中R f，R g，Rh和R 1独立地选自氢，低级烷基，烷氧基，卤素和三氟甲基，并且R 8是氢或-C（O） R“其中R”为低级烷基，烷氧基，苄氧基或苯基，其中苯环未被取代或被一个，两个或三个独立地选自低级烷基，三氟甲基，烷氧基和卤素的取代基取代; 或其酸加成盐。

公开(公告)号：US5491253A

公开(公告)日：1996-02-13

申请号：US281502

申请日：1994-07-27

申请人： Timothy L. Stuk ,  Michael S. Allen ,  Anthony R. Haight ,  Francis A. Kerdesky ,  Denton C. Langridge ,  M. Robert Leanna ,  Linda M. Lijewski ,  Laura Melcher ,  Howard E. Morton ,  Daniel W. Norbeck ,  Daniel S. Reno ,  Timothy A. Robbins ,  David Scarpetti ,  Hing L. Sham ,  Thomas J. Sowin ,  Jien-Heh J. Tien ,  Chen Zhao

发明人： Timothy L. Stuk ,  Michael S. Allen ,  Anthony R. Haight ,  Francis A. Kerdesky ,  Denton C. Langridge ,  M. Robert Leanna ,  Linda M. Lijewski ,  Laura Melcher ,  Howard E. Morton ,  Daniel W. Norbeck ,  Daniel S. Reno ,  Timothy A. Robbins ,  David Scarpetti ,  Hing L. Sham ,  Thomas J. Sowin ,  Jien-Heh J. Tien ,  Chen Zhao

IPC分类号： C07C213/00 ,  C07C215/28 ,  C07C225/16 ,  C07C227/18 ,  C07C229/36 ,  C07C231/12 ,  C07C233/35 ,  C07C251/40 ,  C07C255/27 ,  C07C255/42 ,  C07C269/06 ,  C07C271/20 ,  C07D209/44 ,  C07D221/14 ,  C07C261/00 ,  C07C233/00

CPC分类号： C07D221/14 ,  C07C213/00 ,  C07C215/28 ,  C07C225/16 ,  C07C251/40 ,  C07C255/42 ,  C07C269/06 ,  C07C271/20 ,  C07D209/44 ,  C07B2200/07

摘要： Intermediates and processes are disclosed which are useful for the preparation of a substantially pure compound of the formula: ##STR1## wherein R.sub.6 and R.sub.7 are each hydrogen or R.sub.6 and R.sub.7 are independently selected from ##STR2## wherein R.sub.a and R.sub.b are independently selected from hydrogen, loweralkyl and phenyl and R.sub.c, R.sub.d and R.sub.e are independently selected from hydrogen, loweralkyl, trifluoromethyl, alkoxy, halo and phenyl; and ##STR3## wherein the naphthyl ring is unsubstituted or substituted with one, two or three substitutents independently selected from loweralkyl, trifluoromethyl, alkoxy and halo; orR.sub.6 is as defined above and R.sub.7 is R.sub.7a OC(O)--wherein R.sub.7a is loweralkyl or benzyl; orR.sub.6 and R.sub.7 taken together with the nitrogen atom to which they are bonded are ##STR4## wherein R.sub.f, R.sub.g, R.sub.h and R.sub.i are independently selected from hydrogen, loweralkyl, alkoxy, halogen and trifluoromethyl and R.sub.8 is hydrogen or --C(O)R" wherein R" is loweralkyl, alkoxy, benzyloxy or phenyl wherein the phenyl ring is unsubstituted or substituted with one, two or three substituents independently selected from loweralkyl, trifluoromethyl, alkoxy and halo; or an acid addition salt thereof.

摘要翻译： 公开了用于制备基本上纯的下式化合物的中间体和方法：其中R 6和R 7各自为氢或R 6和R 7独立地选自（ⅰ）其中R a和R b独立地为 选自氢，低级烷基和苯基，R c，R d和R e独立地选自氢，低级烷基，三氟甲基，烷氧基，卤素和苯基; （ii）其中萘基环是未取代的或被一个，两个或三个独立地选自低级烷基，三氟甲基，烷氧基和卤素的取代基取代; 或R 6如上所定义，且R 7为R 7 a OC（O） - 其中R 7a为低级烷基或苄基; 其中R f，R g，Rh和R 1独立地选自氢，低级烷基，烷氧基，卤素和三氟甲基，并且R 8是氢或-C（O） R“其中R”为低级烷基，烷氧基，苄氧基或苯基，其中苯环未被取代或被一个，两个或三个独立地选自低级烷基，三氟甲基，烷氧基和卤素的取代基取代; 或其酸加成盐。

公开(公告)号：US5565418A

公开(公告)日：1996-10-15

申请号：US417304

申请日：1995-04-05

申请人： Dale J. Kempf ,  Daniel W. Norbeck ,  Hing L. Sham ,  Chen Zhao ,  Thomas J. Sowin ,  Daniel S. Reno ,  Michael S. Allen ,  Arthur J. Copper ,  Jien-Heh J. Tien

发明人： Dale J. Kempf ,  Daniel W. Norbeck ,  Hing L. Sham ,  Chen Zhao ,  Thomas J. Sowin ,  Daniel S. Reno ,  Michael S. Allen ,  Arthur J. Copper ,  Jien-Heh J. Tien

IPC分类号： A61K31/425 ,  A61K31/427 ,  A61K38/00 ,  A61K45/06 ,  C07C33/46 ,  C07C43/164 ,  C07C43/174 ,  C07C43/205 ,  C07C43/215 ,  C07C43/23 ,  C07C43/30 ,  C07C43/315 ,  C07C45/00 ,  C07C45/29 ,  C07C45/56 ,  C07C45/59 ,  C07C45/62 ,  C07C45/67 ,  C07C45/74 ,  C07C53/134 ,  C07C69/34 ,  C07C69/65 ,  C07C69/732 ,  C07C211/27 ,  C07C215/18 ,  C07C215/20 ,  C07C215/28 ,  C07C229/08 ,  C07C229/26 ,  C07C229/34 ,  C07C233/36 ,  C07C233/40 ,  C07C235/10 ,  C07C235/12 ,  C07C235/34 ,  C07C235/78 ,  C07C237/10 ,  C07C237/20 ,  C07C237/22 ,  C07C239/10 ,  C07C239/18 ,  C07C239/20 ,  C07C247/10 ,  C07C251/40 ,  C07C271/20 ,  C07C271/22 ,  C07C271/34 ,  C07C275/16 ,  C07C275/24 ,  C07C311/03 ,  C07C311/13 ,  C07C311/18 ,  C07C317/10 ,  C07C317/28 ,  C07C317/44 ,  C07C323/12 ,  C07C323/25 ,  C07C381/00 ,  C07D207/08 ,  C07D207/24 ,  C07D209/42 ,  C07D211/62 ,  C07D213/26 ,  C07D213/30 ,  C07D213/34 ,  C07D213/40 ,  C07D213/54 ,  C07D213/56 ,  C07D213/61 ,  C07D213/75 ,  C07D233/54 ,  C07D233/84 ,  C07D235/14 ,  C07D235/16 ,  C07D239/26 ,  C07D241/12 ,  C07D261/08 ,  C07D263/32 ,  C07D277/24 ,  C07D277/28 ,  C07D277/30 ,  C07D277/34 ,  C07D277/36 ,  C07D277/40 ,  C07D277/42 ,  C07D277/56 ,  C07D295/13 ,  C07D295/205 ,  C07D295/215 ,  C07D303/36 ,  C07D307/42 ,  C07D333/16 ,  C07D401/12 ,  C07D413/12 ,  C07D417/12 ,  C07D521/00 ,  C07K5/06 ,  C07K5/065

CPC分类号： C07D207/08 ,  A61K31/425 ,  A61K31/427 ,  A61K45/06 ,  C07C211/27 ,  C07C215/18 ,  C07C215/20 ,  C07C215/28 ,  C07C229/08 ,  C07C229/26 ,  C07C229/34 ,  C07C233/36 ,  C07C233/40 ,  C07C235/10 ,  C07C235/12 ,  C07C235/34 ,  C07C235/78 ,  C07C237/10 ,  C07C237/20 ,  C07C237/22 ,  C07C239/10 ,  C07C239/18 ,  C07C239/20 ,  C07C247/10 ,  C07C251/40 ,  C07C271/20 ,  C07C271/22 ,  C07C271/34 ,  C07C275/16 ,  C07C275/24 ,  C07C311/03 ,  C07C311/13 ,  C07C311/18 ,  C07C317/10 ,  C07C317/28 ,  C07C317/44 ,  C07C323/12 ,  C07C323/25 ,  C07C33/46 ,  C07C381/00 ,  C07C43/164 ,  C07C43/1742 ,  C07C43/2055 ,  C07C43/215 ,  C07C43/23 ,  C07C43/30 ,  C07C43/315 ,  C07C45/004 ,  C07C45/29 ,  C07C45/567 ,  C07C45/59 ,  C07C45/62 ,  C07C45/673 ,  C07C45/74 ,  C07C53/134 ,  C07C69/34 ,  C07C69/65 ,  C07C69/732 ,  C07D207/24 ,  C07D209/42 ,  C07D211/62 ,  C07D213/26 ,  C07D213/30 ,  C07D213/34 ,  C07D213/40 ,  C07D213/54 ,  C07D213/56 ,  C07D213/61 ,  C07D213/75 ,  C07D231/12 ,  C07D233/56 ,  C07D233/64 ,  C07D233/84 ,  C07D235/14 ,  C07D235/16 ,  C07D239/26 ,  C07D241/12 ,  C07D249/08 ,  C07D261/08 ,  C07D263/32 ,  C07D277/24 ,  C07D277/28 ,  C07D277/30 ,  C07D277/34 ,  C07D277/36 ,  C07D277/40 ,  C07D277/42 ,  C07D277/56 ,  C07D295/13 ,  C07D295/205 ,  C07D295/215 ,  C07D303/36 ,  C07D307/42 ,  C07D333/16 ,  C07D401/12 ,  C07D413/12 ,  C07D417/12 ,  C07K5/06026 ,  C07K5/06078 ,  A61K38/00

摘要： A retroviral protease inhibiting compound of the formula: ##STR1## is disclosed.

公开(公告)号：US06417366B2

公开(公告)日：2002-07-09

申请号：US09518392

申请日：2000-03-03

申请人： Michael S. Allen ,  Ramiya H. Premchandran ,  Sou-Jen Chang ,  Stephen Condon ,  John A. DeMattei ,  Steven A. King ,  Lawrence Kolaczkowski ,  Sukumar Manna ,  Paul J. Nichols ,  Hemant H. Patel ,  Subhash R. Patel ,  Daniel J. Plata ,  Eric J. Stoner ,  Jien-Heh J. Tien ,  Steven J. Wittenberger

发明人： Michael S. Allen ,  Ramiya H. Premchandran ,  Sou-Jen Chang ,  Stephen Condon ,  John A. DeMattei ,  Steven A. King ,  Lawrence Kolaczkowski ,  Sukumar Manna ,  Paul J. Nichols ,  Hemant H. Patel ,  Subhash R. Patel ,  Daniel J. Plata ,  Eric J. Stoner ,  Jien-Heh J. Tien ,  Steven J. Wittenberger

IPC分类号： C07D21516

CPC分类号： C07D215/14 ,  C07C68/06 ,  C07C69/96

摘要： The invention relates to a process for preparing quinoline-substituted carbonate and carbamate compounds, which are important intermediates in the synthesis of 6-O-substituted macrolide antibiotics. The process employs metal-catalyzed coupling reactions to provide a carbonate or carbamate of formula (I) or (II) or a substrate that can be reduced to obtain the same.

摘要翻译： 本发明涉及制备喹啉取代的碳酸酯和氨基甲酸酯化合物的方法，其是合成6-O-取代的大环内酯类抗生素的重要中间体。 该方法使用金属催化的偶联反应来提供式（I）或（II）的碳酸酯或氨基甲酸酯或可以还原得到相同的底物。

公开(公告)号：US5786500A

公开(公告)日：1998-07-28

申请号：US623066

申请日：1996-03-28

申请人： Michael S. Allen ,  Jien-Heh J. Tien

发明人： Michael S. Allen ,  Jien-Heh J. Tien

IPC分类号： C07C215/28 ,  C07C269/06 ,  C07C269/08 ,  C07C271/20 ,  C07C26/100

CPC分类号： C07C269/06 ,  C07C269/08 ,  C07B2200/07

摘要： Intermediates and processes are disclosed which are useful for the preparation of a substantially pure compound of the formula: ##STR1## wherein R.sub.6 and R.sub.7 are each hydrogen or R.sub.6 and R.sub.7 are independently selected from ##STR2## wherein R.sub.a and R.sub.b are independently selected from hydrogen, loweralkyl and phenyl and R.sub.c, R.sub.d and R.sub.e are independently selected from hydrogen, loweralkyl, trifluoromethyl, alkoxy, halo and phenyl; and ##STR3## wherein the naphthyl ring is unsubstituted or substituted with one, two or three substituents independently selected from loweralkyl, trifluoromethyl, alkoxy and halo; or R.sub.6 is as defined above and R.sub.7 is R.sub.7a OC(O)-- wherein R.sub.7a is loweralkyl or benzyl; or R.sub.6 and R.sub.7 taken together with the nitrogen atom to which they are bonded are ##STR4## wherein R.sub.f, R.sub.g, R.sub.h and R.sub.i are independently selected from hydrogen, loweralkyl, alkoxy, halogen and trifluoromethyl and R.sub.8 is hydrogen or --C(O)R" wherein R" is loweralkyl, alkoxy, benzyloxy or phenyl wherein the phenyl ring is unsubstituted or substituted with one, two or three substituents independently selected from loweralkyl, trifluoromethyl, alkoxy and halo; or an acid addition salt thereof.

摘要翻译： 公开了用于制备基本上纯的下式化合物的中间体和方法：其中R 6和R 7各自为氢或R 6和R 7独立地选自（ⅰ）其中R a和R b独立地为 选自氢，低级烷基和苯基，R c，R d和R e独立地选自氢，低级烷基，三氟甲基，烷氧基，卤素和苯基; （ii）其中萘基环是未取代的或被一个，两个或三个独立地选自低级烷基，三氟甲基，烷氧基和卤素的取代基取代; 或R 6如上所定义，R 7为R 7aa（O） - ，其中R 7a为低级烷基或苄基; 其中R f，R g，Rh和R 1独立地选自氢，低级烷基，烷氧基，卤素和三氟甲基，并且R 8是氢或-C （O）R“其中R”是低级烷基，烷氧基，苄氧基或苯基，其中苯环是未取代的或被一个，两个或三个独立地选自低级烷基，三氟甲基，烷氧基和卤素的取代基取代; 或其酸加成盐。

公开(公告)号：US5654466A

公开(公告)日：1997-08-05

申请号：US625783

申请日：1996-02-29

申请人： Timothy L. Stuk ,  Michael S. Allen ,  Anthony R. Haight ,  Howard E. Morton ,  Daniel S. Reno ,  Hing Leung Sham ,  Thomas J. Sowin ,  Jien-Heh J. Tien

发明人： Timothy L. Stuk ,  Michael S. Allen ,  Anthony R. Haight ,  Howard E. Morton ,  Daniel S. Reno ,  Hing Leung Sham ,  Thomas J. Sowin ,  Jien-Heh J. Tien

IPC分类号： C07C213/00 ,  C07C215/28 ,  C07C225/16 ,  C07C227/18 ,  C07C229/36 ,  C07C231/12 ,  C07C233/35 ,  C07C251/40 ,  C07C255/27 ,  C07C255/42 ,  C07C269/06 ,  C07C271/20 ,  C07D209/44 ,  C07D221/14 ,  C07C261/00 ,  C07C233/00 ,  C07D209/04

CPC分类号： C07D221/14 ,  C07C213/00 ,  C07C215/28 ,  C07C225/16 ,  C07C251/40 ,  C07C255/42 ,  C07C269/06 ,  C07C271/20 ,  C07D209/44 ,  C07B2200/07

摘要： Intermediates and processes are disclosed which are useful for the preparation of a substantially pure compound of the formula: ##STR1## wherein R.sub.6 and R.sub.7 are each hydrogen or R.sub.6 and R.sub.7 are independently selected from ##STR2## wherein R.sub.a and R.sub.b are independently selected from hydrogen, loweralkyl and phenyl and R.sub.c, R.sub.d and R.sub.e are independently selected from hydrogen, loweralkyl, trifluoromethyl, alkoxy, halo and phenyl; and ##STR3## wherein the naphthyl ring is unsubstituted or substituted with one, two or three substitutents independently selected from loweralkyl, trifluoromethyl, alkoxy and halo; orR.sub.6 is as defined above and R.sub.7 is R.sub.7a OC(O)-- wherein R.sub.7a is loweralkyl or benzyl; orR.sub.6 and R.sub.7 taken together with the nitrogen atom to which they are bonded are ##STR4## wherein R.sub.f, R.sub.g, R.sub.h and R.sub.i are independently selected from hydrogen, loweralkyl, alkoxy, halogen and trifluoromethyl and R.sub.8 is hydrogen or --C(O)R" wherein R" is loweralkyl, alkoxy, benzyloxy or phenyl wherein the phenyl ring is unsubstituted or substituted with one, two or three substituents independently selected from loweralkyl, trifluoromethyl, alkoxy and halo; or an acid addition salt thereof.

摘要翻译： 公开了用于制备基本上纯的下式化合物的中间体和方法：其中R 6和R 7各自为氢或R 6和R 7独立地选自（ⅰ）其中R a和R b独立地为 选自氢，低级烷基和苯基，R c，R d和R e独立地选自氢，低级烷基，三氟甲基，烷氧基，卤素和苯基; （ii）其中萘基环是未取代的或被一个，两个或三个独立地选自低级烷基，三氟甲基，烷氧基和卤素的取代基取代; 或R 6如上所定义，R 7为R 7aa（O） - ，其中R 7a为低级烷基或苄基; 其中R f，R g，Rh和R 1独立地选自氢，低级烷基，烷氧基，卤素和三氟甲基，并且R 8是氢或-C（O） R“其中R”为低级烷基，烷氧基，苄氧基或苯基，其中苯环未被取代或被一个，两个或三个独立地选自低级烷基，三氟甲基，烷氧基和卤素的取代基取代; 或其酸加成盐。

公开(公告)号：US5625092A

公开(公告)日：1997-04-29

申请号：US419168

申请日：1995-04-10

申请人： Timothy L. Stuk ,  Michael S. Allen ,  Anthony R. Haight ,  Francis A. J. Kerdesky ,  Denton C. Langridge ,  M. Robert Leanna ,  Linda M. Lijewski ,  Laura Melcher ,  Howard E. Morton ,  Daniel W. Norbeck ,  Daniel S. Reno ,  Timothy A. Robbins ,  David Scarpetti ,  Hing L. Sham ,  Thomas J. Sowin ,  Jien-Heh J. Tien ,  Chen Zhao

发明人： Timothy L. Stuk ,  Michael S. Allen ,  Anthony R. Haight ,  Francis A. J. Kerdesky ,  Denton C. Langridge ,  M. Robert Leanna ,  Linda M. Lijewski ,  Laura Melcher ,  Howard E. Morton ,  Daniel W. Norbeck ,  Daniel S. Reno ,  Timothy A. Robbins ,  David Scarpetti ,  Hing L. Sham ,  Thomas J. Sowin ,  Jien-Heh J. Tien ,  Chen Zhao

IPC分类号： C07C213/00 ,  C07C215/28 ,  C07C225/16 ,  C07C227/18 ,  C07C229/36 ,  C07C231/12 ,  C07C233/35 ,  C07C251/40 ,  C07C255/27 ,  C07C255/42 ,  C07C269/06 ,  C07C271/20 ,  C07D209/44 ,  C07D221/14 ,  C07C261/00 ,  C07C233/00 ,  C07D209/04

CPC分类号： C07D221/14 ,  C07C213/00 ,  C07C215/28 ,  C07C225/16 ,  C07C251/40 ,  C07C255/42 ,  C07C269/06 ,  C07C271/20 ,  C07D209/44 ,  C07B2200/07

摘要： Intermediates and processes are disclosed which are useful for the preparation of a substantially pure compound of the formula: ##STR1## wherein R.sub.6 and R.sub.7 are each hydrogen or R.sub.6 and R.sub.7 are independently selected from ##STR2## wherein R.sub.a and R.sub.b are independently selected from hydrogen, loweralkyl and phenyl and R.sub.c, R.sub.d and R.sub.e are independently selected from hydrogen, loweralkyl, trifluoromethyl, alkoxy, halo and phenyl; and ##STR3## wherein the naphthyl ring is unsubstituted or substituted with one, two or three substitutents independently selected from loweralkyl, trifluoromethyl, alkoxy and halo; orR.sub.6 is as defined above and R.sub.7 is R.sub.7a OC(O)-- wherein R.sub.7a is loweralkyl or benzyl; orR.sub.6 and R.sub.7 taken together with the nitrogen atom to which they are bonded are ##STR4## wherein R.sub.f, R.sub.g, R.sub.h and R.sub.i are independently selected from hydrogen, loweralkyl, alkoxy, halogen and trifluoromethyl and R.sub.8 is hydrogen or --C(O)R" wherein R" is loweralkyl, alkoxy, benzyloxy or phenyl wherein the phenyl ring is unsubstituted or substituted with one, two or three substituents independently selected from loweralkyl, trifluoromethyl, alkoxy and halo; or an acid addition salt thereof.

摘要翻译： 公开了用于制备基本上纯的下式化合物的中间体和方法：其中R 6和R 7各自为氢或R 6和R 7独立地选自（ⅰ）其中R a和R b独立地为 选自氢，低级烷基和苯基，R c，R d和R e独立地选自氢，低级烷基，三氟甲基，烷氧基，卤素和苯基; （ii）其中萘基环是未取代的或被一个，两个或三个独立地选自低级烷基，三氟甲基，烷氧基和卤素的取代基取代; 或R 6如上所定义，R 7为R 7aa（O） - ，其中R 7a为低级烷基或苄基; 其中R f，R g，Rh和R 1独立地选自氢，低级烷基，烷氧基，卤素和三氟甲基，并且R 8是氢或-C（O） R“其中R”为低级烷基，烷氧基，苄氧基或苯基，其中苯环未被取代或被一个，两个或三个独立地选自低级烷基，三氟甲基，烷氧基和卤素的取代基取代; 或其酸加成盐。