公开(公告)号：EP1192139B1

公开(公告)日：2012-04-18

申请号：EP00942823.6

申请日：2000-06-15

申请人： ABBOTT LABORATORIES

发明人： ALLEN, Michael, S. ,  PREMCHANDRAN, Ramiya, H. ,  CHANG, Sou-Jen ,  CONDON, Stephen ,  DEMATTEI, John, J. ,  KING, Steven, A. ,  KOLACZKOWSKI, Lawrence ,  MANNA, Sukumar ,  NICHOLS, Paul J. ,  PATEL, Hemant, H. ,  PATEL, Subhash, R. ,  PLATA, Daniel, J. ,  STONER, Eric, J. ,  TIEN, Jien-Heh, J. ,  WITTENBERGER, Steven, J.

IPC分类号： C07D215/14 ,  C07C69/96 ,  C07C68/06 ,  C07C271/12 ,  C07C269/06 ,  C07C43/303 ,  C07C33/03 ,  C07C47/22 ,  C07C57/04

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：EP1007517B1

公开(公告)日：2003-10-08

申请号：EP98942099.7

申请日：1998-08-18

申请人： Abbott Laboratories

发明人： ALLEN, Michael, S.

IPC分类号： C07D277/24 ,  C07D277/22 ,  C07D277/32

CPC分类号： C07D277/22 ,  C07D277/24 ,  C07D277/32

摘要： The present invention discloses a process for the preparation of a hydroxymethylthiazole compound having formula (3). The process of the invention comprises reacting a halomethyl thiazole having formula (A) with water, at an elevated temperature. Optionally, the reaction can be carried out in the presence of a base, such as sodium carbonate, which can react with any acid formed. In the process of the invention, X is a halogen atom; and R6 is selected from the group consisting of hydrogen, and halogen atoms. The invention also contemplates the preparation of acid addition salts of the hydroxymethylthiazole, compound (3).

公开(公告)号：EP1007517A1

公开(公告)日：2000-06-14

申请号：EP98942099.7

申请日：1998-08-18

申请人： Abbott Laboratories

发明人： ALLEN, Michael, S.

IPC分类号： C07D277/24 ,  C07D277/22 ,  C07D277/32

CPC分类号： C07D277/22 ,  C07D277/24 ,  C07D277/32

摘要： The present invention discloses a process for the preparation of a hydroxymethylthiazole compound having formula (3). The process of the invention comprises reacting a halomethyl thiazole having formula (A) with water, at an elevated temperature. Optionally, the reaction can be carried out in the presence of a base, such as sodium carbonate, which can react with any acid formed. In the process of the invention, X is a halogen atom; and R6 is selected from the group consisting of hydrogen, and halogen atoms. The invention also contemplates the preparation of acid addition salts of the hydroxymethylthiazole, compound (3).

公开(公告)号：EP1192139A1

公开(公告)日：2002-04-03

申请号：EP00942823.6

申请日：2000-06-15

申请人： Abbott Laboratories

发明人： ALLEN, Michael, S. ,  PREMCHANDRAN, Ramiya, H. ,  CHANG, Sou-Jen ,  CONDON, Stephen ,  DEMATTEI, John, J. ,  KING, Steven, A. ,  KOLACZKOWSKI, Lawrence ,  MANNA, Sukumar ,  NICHOLS, Paul, J. ,  PATEL, Hemant, H. ,  PATEL, Subhash, R. ,  PLATA, Daniel, J. ,  STONER, Eric, J. ,  TIEN, Jien-Heh, J. ,  WITTENBERGER, Steven, J.

IPC分类号： C07D215/14 ,  C07C69/96 ,  C07C68/06 ,  C07C271/12 ,  C07C269/06 ,  C07C43/303 ,  C07C33/03 ,  C07C47/22 ,  C07C57/04

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：EP0724563B1

公开(公告)日：1999-09-01

申请号：EP94929340.1

申请日：1994-09-26

申请人： ABBOTT LABORATORIES

发明人： STUK, Timothy, L. ,  KERDESKY, Francis, A., J. ,  LIJEWSKI, Linda, M. ,  NORBECK, Daniel, W. ,  SCARPETTI, David ,  TIEN, Jien-Heh, J. ,  ALLEN, Michael, S. ,  LANGRIDGE, Denton, C. ,  MELCHER, Laura ,  RENO, Daniel, S. ,  SHAM, Hing, Leung ,  ZHAO, Chen ,  HAIGHT, Anthony, R. ,  LEANNA, M., Robert ,  MORTON, Howard, E. ,  ROBBINS, Timothy, A. ,  SOWIN, Thomas, J.

IPC分类号： C07C225/16 ,  C07C213/00 ,  C07C255/42 ,  C07C271/20 ,  C07C269/06 ,  C07C215/28 ,  C07C251/40

CPC分类号： C07D221/14 ,  C07B2200/07 ,  C07C213/00 ,  C07C215/28 ,  C07C225/16 ,  C07C251/40 ,  C07C255/42 ,  C07C269/06 ,  C07C271/20 ,  C07D209/44 ,  C07C215/08

摘要： Intermediates and processes are disclosed which are useful for the preparation of a substantially pure compound of formula (3), wherein R6 and R7 are each hydrogen or R6 and R7 are independently selected from (i), wherein Ra and Rb are independently selected from hydrogen, loweralkyl and phenyl and Rc, Rd and Re are independently selected from hydrogen, loweralkyl, trifluoromethyl, alkoxy, halo and phenyl; and (ii) wherein the naphthyl ring is unsubstituted or substituted with one, two or three substituents independently selected from loweralkyl, trifluoromethyl, alkoxy and halo; or R6 is as defined above and R7 is R7aOC (O)-wherein R7a is loweralkyl or benzyl; or R6 and R7 taken together with the nitrogen atom to which they are bonded are (a) or (b), wherein Rf, Rg, Rh and Ri are independently selected from hydrogen, loweralkyl, alkoxy, halogen and trifluoromethyl and R8 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：EP0724563A1

公开(公告)日：1996-08-07

申请号：EP94929340.0

申请日：1994-09-26

申请人： ABBOTT LABORATORIES

发明人： STUK, Timothy, L. ,  KERDESKY, Francis, A., J. ,  LIJEWSKI, Linda, M. ,  NORBECK, Daniel, W. ,  SCARPETTI, David ,  TIEN, Jien-Heh, J. ,  ALLEN, Michael, S. ,  LANGRIDGE, Denton, C. ,  MELCHER, Laura ,  RENO, Daniel, S. ,  SHAM, Hing, Leung ,  ZHAO, Chen ,  HAIGHT, Anthony, R. ,  LEANNA, M., Robert ,  MORTON, Howard, E. ,  ROBBINS, Timothy, A. ,  SOWIN, Thomas, J.

IPC分类号： C07C213 ,  C07C215 ,  C07C225 ,  C07C227 ,  C07C229 ,  C07C231 ,  C07C233 ,  C07C251 ,  C07C255 ,  C07C269 ,  C07C271 ,  C07D209 ,  C07D221

CPC分类号： C07D221/14 ,  C07B2200/07 ,  C07C213/00 ,  C07C215/28 ,  C07C225/16 ,  C07C251/40 ,  C07C255/42 ,  C07C269/06 ,  C07C271/20 ,  C07D209/44 ,  C07C215/08

摘要： Intermediates and processes are disclosed which are useful for the preparation of a substantially pure compound of formula (3), wherein R6 and R7 are each hydrogen or R6 and R7 are independently selected from (i), wherein Ra and Rb are independently selected from hydrogen, loweralkyl and phenyl and Rc, Rd and Re are independently selected from hydrogen, loweralkyl, trifluoromethyl, alkoxy, halo and phenyl; and (ii) wherein the naphthyl ring is unsubstituted or substituted with one, two or three substituents independently selected from loweralkyl, trifluoromethyl, alkoxy and halo; or R6 is as defined above and R7 is R7aOC (O)-wherein R7a is loweralkyl or benzyl; or R6 and R7 taken together with the nitrogen atom to which they are bonded are (a) or (b), wherein Rf, Rg, Rh and Ri are independently selected from hydrogen, loweralkyl, alkoxy, halogen and trifluoromethyl and R8 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.