公开(公告)号：US5284954A

公开(公告)日：1994-02-08

申请号：US954645

申请日：1992-09-30

申请人： Steven J. Wittenberger ,  Bikshandar A. Narayanan ,  Anthony R. Haight ,  David Scarpetti

发明人： Steven J. Wittenberger ,  Bikshandar A. Narayanan ,  Anthony R. Haight ,  David Scarpetti

IPC分类号： C07D239/42 ,  C07D257/04 ,  C07D401/12 ,  C07D403/12 ,  C07D405/14 ,  C07D401/10

CPC分类号： C07D257/04 ,  C07D239/42 ,  C07D401/12 ,  C07D403/12 ,  C07D405/14

摘要： The present invention relates to a process for the preparation of 5-aryl tetrazoles of the formula: ##STR1## or a salt thereof comprising reacting an aryl nitrile with a trisubstituted silyl azide and a disubstituted tin oxide.

摘要翻译： 本发明涉及一种制备下式的5-芳基四唑的方法：（*化学结构*）或其盐，包括使芳基腈与三取代的甲硅烷基叠氮化物和二取代的氧化锡反应。

公开(公告)号：US06437106B1

公开(公告)日：2002-08-20

申请号：US09518281

申请日：2000-03-03

申请人： Eric J. Stoner ,  Matthew J. Peterson ,  Yi-Yin Ku ,  Russell D. Cink ,  Arthur J. Cooper ,  Mahendra N. Deshpande ,  Tim Grieme ,  Anthony R. Haight ,  David R. Hill ,  Margaret Chi-Ping Hsu ,  Steven A. King ,  Marvin Robert Leanna ,  Elaine C. Lee ,  Maureen A. McLaughlin ,  Howard E. Morton ,  James J. Napier ,  Daniel J. Plata ,  Prasad S. Raje ,  Michael Rasmussen ,  David Riley ,  Jien-Heh J. Tien ,  Steven J. Wittenberger

发明人： Eric J. Stoner ,  Matthew J. Peterson ,  Yi-Yin Ku ,  Russell D. Cink ,  Arthur J. Cooper ,  Mahendra N. Deshpande ,  Tim Grieme ,  Anthony R. Haight ,  David R. Hill ,  Margaret Chi-Ping Hsu ,  Steven A. King ,  Marvin Robert Leanna ,  Elaine C. Lee ,  Maureen A. McLaughlin ,  Howard E. Morton ,  James J. Napier ,  Daniel J. Plata ,  Prasad S. Raje ,  Michael Rasmussen ,  David Riley ,  Jien-Heh J. Tien ,  Steven J. Wittenberger

IPC分类号： C07H100

CPC分类号： C07H17/08

摘要： In one aspect, the invention relates to a process for preparing 6-O-substituted erythromycin derivatives comprising reacting 2′-substituted and optionally 4″-substituted 9-oxime erythromycin derivatives with an alkylating agent in the presence of a palladium catalyst and phosphine. In another aspect, the invention relates to processes for preparing 6-O-substituted erythromycin ketolides using the palladium-catalyzed alkylation reaction.

摘要翻译： 一方面，本发明涉及一种制备6-O-取代的红霉素衍生物的方法，其包括在钯催化剂和膦的存在下使2'-取代的和任选的4'-取代的9-肟红霉素衍生物与烷基化剂反应 。 另一方面，本发明涉及使用钯催化的烷基化反应制备6-O-取代的红霉素酮内酯的方法。

公开(公告)号：US08399468B2

公开(公告)日：2013-03-19

申请号：US12715660

申请日：2010-03-02

申请人： Marlon D. Cowart ,  Chen Zhao ,  Minghua Sun ,  Lawrence A. Black ,  Guo Zhu Zheng ,  Robert J. Gregg ,  Geoff G. Z. Zhang ,  Ahmad Y. Sheikh ,  Xiaochun Lou ,  Rodger F. Henry ,  David M. Barnes ,  Lawrence Kolaczkowski ,  Anthony R. Haight ,  Sou-Jen Chang ,  Steven J. Wittenberger ,  Michael G. Fickes

发明人： Marlon D. Cowart ,  Chen Zhao ,  Minghua Sun ,  Lawrence A. Black ,  Guo Zhu Zheng ,  Robert J. Gregg ,  Geoff G. Z. Zhang ,  Ahmad Y. Sheikh ,  Xiaochun Lou ,  Rodger F. Henry ,  David M. Barnes ,  Lawrence Kolaczkowski ,  Anthony R. Haight ,  Sou-Jen Chang ,  Steven J. Wittenberger ,  Michael G. Fickes

IPC分类号： A61K31/501 ,  C07D403/10

CPC分类号： C07D487/04

摘要： Octahydro-pyrrolo[3,4-b]pyrrole derivatives are useful in treating conditions or disorders prevented by or ameliorated by histamine-3 receptor ligands. Octahydro-pyrrolo[3,4-b]pyrrole compounds, methods for using such compounds, compositions for making them, and processes for preparing such compounds are disclosed herein.

摘要翻译： 八氢吡咯并[3,4-b]吡咯衍生物可用于治疗组胺-3受体配体预防或改善的病症或病症。 八氢吡咯并[3,4-b]吡咯化合物，使用这些化合物的方法，制备它们的组合物和制备这些化合物的方法在本文中公开。

公开(公告)号：US20100222358A1

公开(公告)日：2010-09-02

申请号：US12715660

申请日：2010-03-02

申请人： Marlon D. Cowart ,  Chen Zhao ,  Minghua Sun ,  Lawrence A. Black ,  Guo Zhu Zheng ,  Robert J. Gregg ,  Geoff G.Z. Zhang ,  Ahmad Y. Sheikh ,  Xiaochun Lou ,  Rodger F. Henry ,  David M. Barnes ,  Lawrence Kolaczkowski ,  Anthony R. Haight ,  Sou-Jen Chang ,  Steven J. Wittenberger ,  Michael G. Fickes

发明人： Marlon D. Cowart ,  Chen Zhao ,  Minghua Sun ,  Lawrence A. Black ,  Guo Zhu Zheng ,  Robert J. Gregg ,  Geoff G.Z. Zhang ,  Ahmad Y. Sheikh ,  Xiaochun Lou ,  Rodger F. Henry ,  David M. Barnes ,  Lawrence Kolaczkowski ,  Anthony R. Haight ,  Sou-Jen Chang ,  Steven J. Wittenberger ,  Michael G. Fickes

IPC分类号： A61K31/501 ,  A61K31/407 ,  C07D487/04 ,  A61K31/47 ,  C07D215/00 ,  A61K31/4439 ,  C07D401/14 ,  A61K31/428 ,  C07D417/14 ,  A61K31/4164 ,  C07D233/00 ,  C07D403/14 ,  A61K31/506 ,  A61K31/497 ,  A61P3/04 ,  A61P5/00 ,  A61P11/06 ,  A61P25/00 ,  A61P29/00 ,  A61P37/08 ,  A61P1/02

CPC分类号： C07D487/04

摘要： Octahydro-pyrrolo[3,4-b]pyrrole derivatives are useful in treating conditions or disorders prevented by or ameliorated by histamine-3 receptor ligands. Octahydro-pyrrolo[3,4-b]pyrrole compounds, methods for using such compounds, compositions for making them, and processes for preparing such compounds are disclosed herein.

摘要翻译： 八氢吡咯并[3,4-b]吡咯衍生物可用于治疗组胺-3受体配体预防或改善的病症或病症。 八氢吡咯并[3,4-b]吡咯化合物，使用这些化合物的方法，制备它们的组合物和制备这些化合物的方法在本文中公开。

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：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。

公开(公告)号：US5569777A

公开(公告)日：1996-10-29

申请号：US418727

申请日：1995-04-07

申请人： Timothy L. Stuk ,  Anthony R. Haight ,  Howard E. Morton ,  Timothy A. Robbins ,  David Scarpetti ,  Jien-Heh J. Tien

发明人： Timothy L. Stuk ,  Anthony R. Haight ,  Howard E. Morton ,  Timothy A. Robbins ,  David Scarpetti ,  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.

公开(公告)号：US5543551A

公开(公告)日：1996-08-06

申请号：US419301

申请日：1995-04-10

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 ,  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：US5616776A

公开(公告)日：1997-04-01

申请号：US418705

申请日：1995-04-07

申请人： Timothy L. Stuk ,  Anthony R. Haight ,  Francis A. J. Kerdesky ,  M. Robert Leanna ,  Howard E. Morton ,  Timothy A. Robbins ,  David Scarpetti ,  Jien-Heh J. Tien

发明人： Timothy L. Stuk ,  Anthony R. Haight ,  Francis A. J. Kerdesky ,  M. Robert Leanna ,  Howard E. Morton ,  Timothy A. Robbins ,  David Scarpetti ,  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

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; 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; 或R 6和R 7与它们所键合的氮原子一起为氢，低级烷基，烷氧基，卤素和三氟甲基，R8为氢或-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：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。