公开(公告)号：US3790560A

公开(公告)日：1974-02-05

申请号：US3790560D

申请日：1972-03-22

申请人： UPJOHN CO

发明人： BANNISTER B

IPC分类号： C07H15/16 ,  C08B19/00

CPC分类号： C07H15/16

摘要： ALKYL 7-DEXY-7-MERCAPTOALKYLTHIO-A-THIOLINCONSAMINIDES USEFUL AS INTERMEDIATES FOR PREPARING ANTIBACTERIALLY ACTIVE 7-DEOXY-7-MERCAPTOALKYLTHIO-LINCOMYCINS ARE PREPARED BY HEATING ALKYL N-ACYL-6,7-AZIRIDINO-6-DEAMINO-7-DEOXY-ATHIOLINCOSAMINIDES WITH AN APPROPRIATE SULFIDE IN THE PRESENCE OF GLACIAL ACETIC ACID OR OTHER ANHYDROUS LOWER ALKANOIC ACID, OR ANHYDROUS BENZOIC ACID OR OTHER ARENOIC ACID OR NOT MORE THAN 12 CARBON ATOMS.

公开(公告)号：US3737425A

公开(公告)日：1973-06-05

申请号：US3737425D

申请日：1970-04-06

申请人： UPJOHN CO

发明人： BANNISTER B

IPC分类号： C07H15/14 ,  C07H15/16 ,  C08B19/00

CPC分类号： C07H15/14 ,  C07H15/16

摘要： ALKYL A-THIOLINCOSAMINIDE IS REACTED WITH PERIODATE TO FORM ALKYL 1-THIO-A-D-GALACTOHEXODIALDO-1,5-PYRANOSIDE, WHICH IS REACTED WITH CYANIDE TO FORM ALKYL 6-CYANO-1-THIOA-D-GALACTOPYRANOSIDE. THE LATTER IS CONVERTED TO ANTIBACTERIALLY ACTIVE 8-NOR-LINECOMYCINS, FIRST THE 3,4-O-POSITIONS ARE COVERED BY AN YLIDENE GROUP. THIS CAN BE DONE INITIALLY BY DEACYLATING ALKYL N-ACETYL-3,4-O-YLIDENE-A-THIOLINOSOMINIDES. THE RESULTING ALKYL 3,4-O-YLIDENE-A-THIOLINCOSAMINIDE IS TREATED SUCCESSIVELY WITH PERIODATE AND CYANIDE. THE ALKYL 6-CYANO-3,4-O-YLIDENE-A-THIOLINCOSAMINIDE IS THEN TOSYLATED AND THE RESULTING 2,7-DI-O-TOSYL DERIVATIVES ARE REDUCED WITH LITHIUM ALUMINUM HYDRIDE TO FORM THE 6,7-AXIRIDINO DERIVATIVE WHICH ON N-ACYLATION AND SOLVOYLIS, DECAYLATION, AND REACYLATION WITH THE ACID MOIETY OF LINCOMYCIN OR AN ANALOG THEREOF, YIELDS THE DESIRED 7-NOR-LINCOMYCIN OR ANALOG THEREOF. WHEN THE SOLVOYLSIS IS AFFECTED WITH METHANOL OR OTHER ALKANOL, ANTIBACTERIALLY ACTIVE 7-O-ALKYL-8-NORLINCOMYCINS ARE OBTAINED.

公开(公告)号：US3767649A

公开(公告)日：1973-10-23

申请号：US3767649D

申请日：1971-11-15

申请人： UPJOHN CO

发明人： BANNISTER B

IPC分类号： C07H15/16 ,  C08B19/00

CPC分类号： C07H15/16

摘要： ALKYL 7-DEOXY-7-RS-A-THIOLINCOSAMINIDES USEFUL AS INTERMEDIATES FOR PREPARING ANTIBACTERIALLY ACTIVE 7-DEOXY7-RS-LINCOMYCINS ARE PREPARED BY HEATING ALKYL N-ACYL6,7 - AZIRIDINO - 6 - DEAMINO-7-DEOXY-A-THIOLINCOSAMINIDES WITH A NON-AROMATIC, CYCLIC MONOSULFIDE IN THE PRESENCE OF GLACIAL ACETIC ACID OR OTHER ANHYDROUS LOWER-ALKANOIC ACID, OR ANHYDROUS BENZOIC ACID OR OTHER ANHYDROUS ARENOIC ACIDS OF NOT MORE THAN 12 CARBON ATOMS.

公开(公告)号：US3764672A

公开(公告)日：1973-10-09

申请号：US3764672D

申请日：1972-02-04

申请人： UPJOHN CO

发明人： KAGAN F ,  MAGERLEIN B ,  ARGOUDELIS A ,  BANNISTER B

IPC分类号： C07H15/16 ,  C08G73/10 ,  A61K21/00

CPC分类号： A61K31/70 ,  C07H15/16 ,  C08G73/1071

摘要： Compounds having the formula v,2/12 WHEREIN R is alkyl of four, five, or six carbon atoms, R1 is methyl or ethyl, and R2 is methyl or ethyl in combination with a pharmaceutical carrier.

摘要翻译： 具有式v，2/12的化合物，其中R是四个，五个或六个碳原子的烷基，R 1是甲基或乙基，R 2是与药物载体组合的甲基或乙基。