公开(公告)号：WO1997010206A1

公开(公告)日：1997-03-20

申请号：PCT/US1996013892

申请日：1996-08-27

Applicant: ABBOTT LABORATORIES

Inventor： ABBOTT LABORATORIES ,  CHEMBURKAR, Sanjay, R. ,  PATEL, Hemantkumar, H. ,  SAWICK, David, P. ,  THOMAS, Albert, V.

IPC: C07C273/18

CPC classification number: C07C43/29 ,  C07C43/295 ,  C07C273/1827 ,  C07C275/64

Abstract: The present invention provides a process for the preparation of a compound of formula (I), wherein R is a straight or branched alkyl group of from one to twelve carbon atoms; M represents hydrogen or a pharmaceutically acceptable cation; and A is selected from optionally substituted carbocyclic phenyl.

Abstract translation: 本发明提供了制备式（I）化合物的方法，其中R是具有1至12个碳原子的直链或支链烷基; M表示氢或药学上可接受的阳离子; 并且A选自任选取代的碳环苯基。

公开(公告)号：WO1998031698A1

公开(公告)日：1998-07-23

申请号：PCT/US1997023356

申请日：1997-12-18

Applicant: ABBOTT LABORATORIES

Inventor： ABBOTT LABORATORIES ,  PAREKH, Shyamal, I. ,  GRAHAM, Alexandra, E. ,  DiPIERRO, Michael, J. ,  THOMAS, Albert, V. ,  RILEY, David, A.

IPC: C07H17/08

CPC classification number: C07H17/08

Abstract: A process for the preparation of 4''-deoxyerythromycins, having formula (I), wherein R is H or OH, Rp is H or acetyl, and R is H or loweralkyl; by treatment of the 2'-O-acetyl-4''-imidazolylthionocarbonyl-erythromycin starting material with the radical initiator 4,4'-azobis-(4-cyanovaleric acid), H3PO2 and an organic base in a water-miscible solvent other than an alcohol, and optionally eliminating the 2'-O-acetyl group. In a preferred embodiment, the water-miscible solvent is an alcohol and the deoxygenation and deacetylation is carried out in one step.

Abstract translation: 制备具有式（I）的4“ - 脱氧红霉素的方法，其中R为H或OH，Rp为H或乙酰基，R 1为H或低级烷基; 通过用自由基引发剂4,4'-偶氮双（4-氰基戊酸），H 3 PO 2和有机碱在水混溶性溶剂中处理2'-O-乙酰基-4“ - 咪唑基硫羰基 - 红霉素原料 并且任选地除去2'-O-乙酰基。 在优选的实施方案中，水混溶性溶剂是醇，脱氧和脱乙酰化在一个步骤中进行。

公开(公告)号：WO1998022488A1

公开(公告)日：1998-05-28

申请号：PCT/US1997020836

申请日：1997-11-17

Applicant: ABBOTT LABORATORIES

Inventor： ABBOTT LABORATORIES ,  PREMCHANDRAN, Ramiya, H. ,  THOMAS, Albert, V. ,  BUSSE, Juliette, K. ,  DETE, John, E.

IPC: C07H17/08

CPC classification number: C07H17/08

Abstract: A process for the preparation of N-demethyl-4"-deoxy-erythromycins A and B, having formula (I), wherein R is H or OH, by stepwise addition of iodine and base to the N-dimethyl-4"-deoxy-erythromycin, preferably, accompanied by sparging with an inert gas.

Abstract translation: 制备具有式（I）的N-脱甲基-4“ - 脱氧 - 红霉素A和B的方法，其中R a是H或OH，通过逐步加入碘和碱向N-二甲基-4 “脱氧红霉素，优选伴随着用惰性气体喷雾。

公开(公告)号：EP1077987A1

公开(公告)日：2001-02-28

申请号：EP97950983.3

申请日：1997-12-18

Applicant: Abbott Laboratories

Inventor： PAREKH, Shyamal, I. ,  GRAHAM, Alexandra, E. ,  DiPIERRO, Michael, J. ,  THOMAS, Albert, V. ,  RILEY, David, A.

IPC: C07H17/08 ,  A61K31/70

CPC classification number: C07H17/08

Abstract: A process for the preparation of 4''-deoxyerythromycins, having formula (I), wherein R is H or OH, Rp is H or acetyl, and R1 is H or loweralkyl; by treatment of the 2'-O-acetyl-4''-imidazolylthionocarbonyl-erythromycin starting material with the radical initiator 4,4'-azobis-(4-cyanovaleric acid), H¿3?PO2 and an organic base in a water-miscible solvent other than an alcohol, and optionally eliminating the 2'-O-acetyl group. In a preferred embodiment, the water-miscible solvent is an alcohol and the deoxygenation and deacetylation is carried out in one step.

Abstract translation: 一种制备具有式（I）的4“ - 脱氧红霉素的方法，其中R是H或OH，Rp是H或乙酰基，R1是H或低级烷基; 通过用自由基引发剂4,4'-偶氮双 - （4-氰基戊酸），H 3 PO 2和有机碱在水中处理2'-O-乙酰基-4“ - 咪唑基硫羰基 - 红霉素原料 与醇不同的溶剂，并且任选地除去2'-O-乙酰基。 在一个优选的实施方案中，水混溶性溶剂是醇并且脱氧和脱乙酰一步进行。

公开(公告)号：EP0850217A1

公开(公告)日：1998-07-01

申请号：EP96931435.0

申请日：1996-08-27

Applicant: Abbott Laboratories

Inventor： CHEMBURKAR, Sanjay, R. ,  PATEL, Hemantkumar H., Apartment 112 ,  SAWICK, David, P. ,  THOMAS, Albert, V.

IPC: C07C43 ,  C07C273 ,  C07C275

CPC classification number: C07C43/29 ,  C07C43/295 ,  C07C273/1827 ,  C07C275/64

Abstract: The present invention provides a process for the preparation of a compound of formula (I), wherein R is a straight or branched alkyl group of from one to twelve carbon atoms; M represents hydrogen or a pharmaceutically acceptable cation; and A is selected from optionally substituted carbocyclic phenyl.

公开(公告)号：EP1077987B1

公开(公告)日：2004-04-28

申请号：EP97950983.3

申请日：1997-12-18

Applicant: Abbott Laboratories

Inventor： PAREKH, Shyamal, I. ,  GRAHAM, Alexandra, E. ,  DiPIERRO, Michael, J. ,  THOMAS, Albert, V. ,  RILEY, David, A.

IPC: C07H17/08 ,  A61K31/70

CPC classification number: C07H17/08

Abstract: A process for the preparation of 4''-deoxyerythromycins, having formula (I), wherein R is H or OH, Rp is H or acetyl, and R is H or loweralkyl; by treatment of the 2'-O-acetyl-4''-imidazolylthionocarbonyl-erythromycin starting material with the radical initiator 4,4'-azobis-(4-cyanovaleric acid), H3PO2 and an organic base in a water-miscible solvent other than an alcohol, and optionally eliminating the 2'-O-acetyl group. In a preferred embodiment, the water-miscible solvent is an alcohol and the deoxygenation and deacetylation is carried out in one step.

Abstract translation: 一种制备具有式（I）的4“ - 脱氧红霉素的方法，其中R是H或OH，Rp是H或乙酰基，并且R 1是H或低级烷基; 通过用自由基引发剂4,4'-偶氮双 - （4-氰基戊酸），H 3 PO 2和有机碱在水混溶性溶剂中处理2'-O-乙酰基-4“ - 咪唑基硫羰基 - 红霉素原料 比醇，并且任选地消除2'-O-乙酰基。 在一个优选的实施方案中，水混溶性溶剂是醇并且脱氧和脱乙酰一步进行。

公开(公告)号：EP0850217B1

公开(公告)日：2000-04-05

申请号：EP96931435.0

申请日：1996-08-27

Applicant: Abbott Laboratories

Inventor： CHEMBURKAR, Sanjay, R. ,  PATEL, Hemantkumar H., Apartment 112 ,  SAWICK, David, P. ,  THOMAS, Albert, V.

IPC: C07C273/18 ,  C07C275/64

CPC classification number: C07C43/29 ,  C07C43/295 ,  C07C273/1827 ,  C07C275/64

Abstract: The present invention provides a process for the preparation of a compound of formula (I), wherein R is a straight or branched alkyl group of from one to twelve carbon atoms; M represents hydrogen or a pharmaceutically acceptable cation; and A is selected from optionally substituted carbocyclic phenyl.