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1. 发明授权

US3928331A Process for the manufacture of 7-amino-3-cephem-4-carboxylic acid derivatives 失效
标题翻译：制备7-氨基-3-头孢烯-4-羧酸衍生物的方法
公开(公告)号：US3928331A
公开(公告)日：1975-12-23
申请号：US39287773
申请日：1973-08-30
申请人： HOECHST AG
发明人： BAUERSCHMIDT EBERHARD , BORMANN DIETER , WORM MANFRED
IPC分类号： C07D501/04 , C07D20060101 , C07D501/16 , C07D501/18
CPC分类号： C07D499/00
摘要： Process for the manufacture of 7-amino-3-cephem-4-carboxylic acids and the esters thereof of the formula I

in which A stands for hydrogen, alkyl, acyloxy, alkyloxy or hydroxy and R stands for hydrogen, optionally substituted linear or branched alkyl, cycloalkyl, aryl, aralkyl, aryloxyalkyl, alkoxyalkyl, acryloxyalkyl, aroylalkyl, or a heterocyclic radical and the salts thereof which comprises reacting 7-acylamino-3cephem-4-carboxylic acid esters of the general formula II

in which R'' stands for optionally substituted alkyl, aryl, aralkyl, aryloxyalkyl, alkoxyalkyl or a heterocyclic radical and R'''' has the meaning given for R but cannot stand for hydrogen and A is defined as above, in an inert solvent with a silylating agent in the presence of a base, converting the amido group activated by the silylation into the iminohalide by adding a halogenating agent, allowing it to react with an alcohol to yield the iminoether hydrohalide, hydrolyzing the iminoether hydrohalide and optionally splitting the 7-amino-3-cephem-4carboxylic acid ester of the general formula I to yield the free acid, the esters obtained being valuable intermediates.
摘要翻译：制备7-氨基-3-头孢烯-4-羧酸的方法及其分子式Ⅰ的酯，其中A代表氢，烷基，酰氧基，烷氧基或羟基，R代表氢，任选取代的直链或支链烷基，环烷基，芳基，芳烷基，芳氧基烷基，烷氧基烷基，丙烯酰氧基烷基，芳酰基烷基或杂环基及其盐，其包括使通式II的7-酰基氨基-3-头孢烯-4-羧酸酯与R' 对于任选取代的烷基，芳基，芳烷基，芳氧基烷基，烷氧基烷基或杂环基，R“具有R给出的含义，但不能代表氢，A如上所定义，在惰性溶剂中，在甲硅烷基化剂存在下，碱，通过加入卤化剂将通过甲硅烷基活化的酰氨基转化成亚胺基卤化物，使其与醇反应得到亚氨基醚氢卤酸盐，水解亚氨基醚氢卤酸盐和任选的制备通式I的7-氨基-3-头孢烯-4-羧酸酯，得到游离酸，得到的酯是有价值的中间体。

2. 发明授权

US3920640A Acylamino-cephem-carboxylic acids and process for preparing them 失效
标题翻译：酰氨基 - 头孢烯羧酸及其制备方法
公开(公告)号：US3920640A
公开(公告)日：1975-11-18
申请号：US35646673
申请日：1973-05-02
申请人： HOECHST AG
发明人： SCHORR MANFRED , WORM MANFRED , SCHRINNER ELMAR
IPC分类号： C07D233/22 , C07D233/26 , C07D239/06 , C07D333/38 , C07D501/20 , C07D501/22 , C07D501/24
CPC分类号： C07D239/06 , C07D233/22 , C07D233/26 , C07D333/38
摘要： IN WHICH R1, R2 and R3 represent hydrogen or lower alkyl groups and R1 and R2 may form together an alkylene group which may be substituted, R4 represents a linear or branched alkyl radical of 1 to 5 carbon atoms, a cyclo-alkyl radical of 3 to 7 carbon atoms which may be interrupted by heteroatoms, X represents a single bond or NH, A represents a phenylene or thienylene group which may be substituted and Y represents a single bond or oxygen, and their physiologically tolerated salts; the novel compounds have very good anti-bacterial properties.

Acylamino-cephem-carboxylic acids of the general formula
摘要翻译：酰基氨基 - 头孢烯羧酸，其通式为R 1，R 2和R 3表示氢或低级烷基，R 1和R 2可以一起形成可被取代的亚烷基，R 4表示1至5的直链或支链烷基碳原子，可被杂原子中断的3-7个碳原子的环烷基，X表示单键或NH，A表示可被取代的亚苯基或亚噻吩基，Y表示单键或氧，以及他们的生理耐受盐; 新型化合物具有非常好的抗菌性能。

3. 发明专利

HUT74296A PROCESS FOR PRODUCE AROMATIC METHYLSULPHONYL DERIVATIVES DURING METHYLIZATION OF ARYL-SULPHINACIDS 未知
公开(公告)号：HUT74296A
公开(公告)日：1996-11-28
申请号：HU9503598
申请日：1995-12-15
申请人： HOECHST AG
发明人： FUELLING GERD , HOERLEIN ROLF , LERCH ULRICH , WORM MANFRED
IPC分类号： C07C313/02 , C07C315/00 , C07C315/02 , C07C317/44 , C07C317/14 , C07D227/00 , C07D273/00

4. 发明专利

FI84829B 未知
公开(公告)号：FI84829B
公开(公告)日：1991-10-15
申请号：FI864886
申请日：1986-12-01
申请人： HOECHST AG
发明人： JAENICKE OTTMAR , WAGNER HANS , WORM MANFRED
IPC分类号： C07D501/06 , A61K20060101 , A61K31/545 , C07D20060101 , C07D501/00 , C07D501/04 , C07D501/36 , C07D501/46 , C07D501/56
摘要： A process for the preparation of cefodizime of the formula +TR wherein (a) a compound of the formula II (ATS) wherein R1 represents hydrogen or an aminoprotective group and A represents a hydrogen atom or one equivalent of an alkali metal or alkaline earth metal, of ammonium or of an organic nitrogen base, is first reacted with a compound of the formula III R-SO2Hal wherein R represents an optionally substituted alkyl, aryl or aralkyl radical and Hal represents a halogen atom, in an organic solvent and, if appropriate, in the presence of a base, (b) a compound of the formula I (TACS) in which A has the above meaning, is reacted with a silylating agent in an organic solvent and, if appropriate, in the presence of a base, and (c) the two products formed in (a) and (b) are reacted in their reaction solutions, and any protective group R1 present in the end product of the formula I is eliminated.

5. 发明专利

CA1287347C PROCESS FOR THE PREPARATION OF CEFODIZIME 未知
公开(公告)号：CA1287347C
公开(公告)日：1991-08-06
申请号：CA524381
申请日：1986-12-02
申请人： HOECHST AG
发明人： JAENICKE OTTMAR , WAGNER HANS , WORM MANFRED
IPC分类号： C07D501/06 , A61K20060101 , A61K31/545 , C07D20060101 , C07D501/00 , C07D501/04 , C07D501/36 , C07D501/46 , C07D501/56
摘要： of the disclosure The invention relates to a process for the preparation of cefodizime of the formula (cefodizime) wherein (a) a compound of the formula II (ATS) wherein R1 represents-hydrogen or an aminoprotective group and A represents a hydrogen atom or one equivalent of an alkali metal or alkaline earth metal, of ammonium or of an organic nitrogen base, is first reacted with a compound of the formula III R-SO2-Hal wherein R represents an alkyl, aryl or aralkyl radical which may be substituted and Hal represents a halogen atom, in an organic solvent and, if appropriate, in the presence of a base, (b) a compound of the formula I (TACS) in which A has the above meaning, is reacted with a silylating agent in an organic solvent and, if appropriate, in the presence of a base, and (c) the two products formed in (a) and (b) are reacted in their reaction solutions, and any protective group R1 present in the end product of the formula I is eliminated.

6. 发明专利

DD252606A5 未知
公开(公告)号：DD252606A5
公开(公告)日：1987-12-23
申请号：DD29691386
申请日：1986-12-01
申请人： HOECHST AG
发明人： JAENICKE OTTMAR , WAGNER HANS , WORM MANFRED
IPC分类号： C07D501/06 , A61K20060101 , A61K31/545 , C07D20060101 , C07D501/00 , C07D501/04 , C07D501/36 , C07D501/46 , C07D501/56
摘要： A process for the preparation of cefodizime of the formula +TR wherein (a) a compound of the formula II (ATS) wherein R1 represents hydrogen or an aminoprotective group and A represents a hydrogen atom or one equivalent of an alkali metal or alkaline earth metal, of ammonium or of an organic nitrogen base, is first reacted with a compound of the formula III R-SO2Hal wherein R represents an optionally substituted alkyl, aryl or aralkyl radical and Hal represents a halogen atom, in an organic solvent and, if appropriate, in the presence of a base, (b) a compound of the formula I (TACS) in which A has the above meaning, is reacted with a silylating agent in an organic solvent and, if appropriate, in the presence of a base, and (c) the two products formed in (a) and (b) are reacted in their reaction solutions, and any protective group R1 present in the end product of the formula I is eliminated.

7. 发明专利

NO864836A 未知
公开(公告)号：NO864836A
公开(公告)日：1987-06-04
申请号：NO864836
申请日：1986-12-02
申请人： HOECHST AG
发明人： JAENICKE OTTMAR , SCHAUINSLAND HANS WAGNER , WORM MANFRED
IPC分类号： C07D501/06 , A61K20060101 , A61K31/545 , C07D20060101 , C07D501/00 , C07D501/04 , C07D501/36 , C07D501/46 , C07D501/56
CPC分类号： C07D501/36 , Y02P20/55

8. 发明专利

NO864836D0 未知
公开(公告)号：NO864836D0
公开(公告)日：1986-12-02
申请号：NO864836
申请日：1986-12-02
申请人： HOECHST AG
发明人： JAENICKE OTTMAR , SCHAUINSLAND HANS WAGNER , WORM MANFRED
IPC分类号： C07D501/06 , A61K20060101 , A61K31/545 , C07D20060101 , C07D501/00 , C07D501/04 , C07D501/36 , C07D501/46 , C07D501/56
摘要： A process for the preparation of cefodizime of the formula +TR wherein (a) a compound of the formula II (ATS) wherein R1 represents hydrogen or an aminoprotective group and A represents a hydrogen atom or one equivalent of an alkali metal or alkaline earth metal, of ammonium or of an organic nitrogen base, is first reacted with a compound of the formula III R-SO2Hal wherein R represents an optionally substituted alkyl, aryl or aralkyl radical and Hal represents a halogen atom, in an organic solvent and, if appropriate, in the presence of a base, (b) a compound of the formula I (TACS) in which A has the above meaning, is reacted with a silylating agent in an organic solvent and, if appropriate, in the presence of a base, and (c) the two products formed in (a) and (b) are reacted in their reaction solutions, and any protective group R1 present in the end product of the formula I is eliminated.

9. 发明专利

AU533578B2 4-PHENYL-1,3-BENZODIAZEPINES 未知
公开(公告)号：AU533578B2
公开(公告)日：1983-12-01
申请号：AU5144679
申请日：1979-10-04
申请人： HOECHST AG
发明人： MARTIN LAWRENCE LEO , WORM MANFRED , CRICHLOW CHARLES ANTHONY
IPC分类号： C07C251/66 , A61K31/135 , A61K31/55 , A61P25/04 , A61P25/08 , A61P25/24 , A61P25/26 , A61P31/04 , C07C67/00 , C07C201/00 , C07C205/45 , C07C209/00 , C07C211/49 , C07C211/52 , C07C213/00 , C07C215/74 , C07C215/80 , C07C217/78 , C07C217/80 , C07C239/00 , C07D243/04 , C07C87/28

10. 发明专利

AU5144679A 4-PHENYL-1,3-BENZODIAZEPINES 未知
公开(公告)号：AU5144679A
公开(公告)日：1980-04-17
申请号：AU5144679
申请日：1979-10-04
申请人： HOECHST AG
发明人： MARTIN LAWRENCE LEO , WORM MANFRED , CRICHLOW CHARLES ANTHONY
IPC分类号： C07C251/66 , A61K31/135 , A61K31/55 , A61P25/04 , A61P25/08 , A61P25/24 , A61P25/26 , A61P31/04 , C07C67/00 , C07C201/00 , C07C205/45 , C07C209/00 , C07C211/49 , C07C211/52 , C07C213/00 , C07C215/74 , C07C215/80 , C07C217/78 , C07C217/80 , C07C239/00 , C07D243/04 , C07C87/28

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