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公开(公告)号:DE2641060A1
公开(公告)日:1978-03-16
申请号:DE2641060
申请日:1976-09-11
Applicant: HOECHST AG
Inventor: SCHORR MANFRED DIPL CHEM DR , SCHRINNER ELMAR DR , WORM MANFRED DIPL CHEM DR , SCHMITT WILFRIED
IPC: C07D235/12 , C07D235/18 , C07D471/04 , C07D499/64 , C07D501/20 , C07D499/70 , A61K31/43 , A61K31/545
Abstract: Beta-Lactam cpds. of formula (I) and their acceptable salts and esters are new. In (I) X is of formula (H) or (J) R1 is H, opt. substd. alkyl, aryl or heterocyclic gp; R2 and R4 are H or lower alkyl; R3 and R5 are H, halogen, lower alkyl or alkoxy; A is CH or N; B is a single bond or methyleneoxy; C is a single bond, or phenylene; D is a single bond, lower alkylene or oxyalkylene; Y is opt. substd. Ph, opt. substd. monocyclic aromatic heterocyclic gp. or dihydrophenyl; and Z is of formula (K) or (L) E is H, acetoxy of S-G; G is an opt. substd. heterocyclic gp.). Typical cpds. are 6 D-2-(4-(benzimidazol-2-yl)phenoxyacetylamino-2-phenyl-acetylami- no -penicillanic acid and 7 D-2-(2-(4-fluorophenyl)-benzimidazol-5-yl-carbonylamino)-2-phen- ylacetyl-amino -cephalosporanic acid.
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公开(公告)号:CA1001616A
公开(公告)日:1976-12-14
申请号:CA171107
申请日:1973-05-04
Applicant: HOECHST AG
Inventor: BORMANN DIETER , SCHORR MANFRED , SCHMITT WILFRIED
IPC: C07D499/04 , C07D499/00 , C07D499/06 , C07D499/10 , C07D499/42 , C07D501/04 , C07D501/18
Abstract: 1431486 Preparing 6-aminopenicillanic acid and 7-aminocephalosporanic acids HOECHST AG 7 May 1973 [5 May 1972] 21586/73 Heading C2C 6-Amino-penicillanic acid and 7-amino-cephalosporanic acids, having the general Formula (I) in which Z is a group (Ia) or (Ib) wherein A is hydrogen or an acyloxy, alkyloxy or hydroxy group, are prepared by reacting a salt of an acylamino-penicillanic or cephalosporanic acid of general Formula (II) wherein Z is a group (Ia) or (Ib) as defined above and R is hydrogen or an unsubstituted or substituted alkyl, aryl, aralkyl, aryloxyalkyl or heterocyclic radical, in an inert solvent under anhydrous conditions with a phosphinic acid halide of Formula (III) wherein R 1 and R 2 are the same or different and each is an alkyl, cycloalkyl or aryl radical, X is oxygen or sulphur, and Hal is a halogen atom, with the proviso that X is not oxygen when A in the group (Ib) is hydrogen, acetoxy or alkyloxy; reacting the resulting mixed anhydride with an imidohalide-forming agent under anhydrous conditions; converting the resulting imidohalide into an imino-ether by reaction with an alcohol; hydrolysing the iminoether with water to give the compound (I), and precipitating this compound from the reaction mixture by adjusting the pH to its isoelectric point.
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公开(公告)号:DE2222094A1
公开(公告)日:1973-11-15
申请号:DE2222094
申请日:1972-05-05
Applicant: HOECHST AG
IPC: C07D499/04 , C07D499/00 , C07D499/06 , C07D499/10 , C07D499/42 , C07D501/04 , C07D501/18 , C07D25/00
Abstract: 1431486 Preparing 6-aminopenicillanic acid and 7-aminocephalosporanic acids HOECHST AG 7 May 1973 [5 May 1972] 21586/73 Heading C2C 6-Amino-penicillanic acid and 7-amino-cephalosporanic acids, having the general Formula (I) in which Z is a group (Ia) or (Ib) wherein A is hydrogen or an acyloxy, alkyloxy or hydroxy group, are prepared by reacting a salt of an acylamino-penicillanic or cephalosporanic acid of general Formula (II) wherein Z is a group (Ia) or (Ib) as defined above and R is hydrogen or an unsubstituted or substituted alkyl, aryl, aralkyl, aryloxyalkyl or heterocyclic radical, in an inert solvent under anhydrous conditions with a phosphinic acid halide of Formula (III) wherein R 1 and R 2 are the same or different and each is an alkyl, cycloalkyl or aryl radical, X is oxygen or sulphur, and Hal is a halogen atom, with the proviso that X is not oxygen when A in the group (Ib) is hydrogen, acetoxy or alkyloxy; reacting the resulting mixed anhydride with an imidohalide-forming agent under anhydrous conditions; converting the resulting imidohalide into an imino-ether by reaction with an alcohol; hydrolysing the iminoether with water to give the compound (I), and precipitating this compound from the reaction mixture by adjusting the pH to its isoelectric point.
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公开(公告)号:DE3536028A1
公开(公告)日:1987-04-09
申请号:DE3536028
申请日:1985-10-09
Applicant: HOECHST AG
Inventor: SCHORR MANFRED DR , SCHMITT WILFRIED
IPC: C07D207/26 , C07D207/267 , C07D211/76 , C07D223/10 , C07D225/02
Abstract: A process for the preparation of 1-substituted azacycloalkan-2-ones of the formula I I in which R, m and n have the meanings indicated by reaction of corresponding 1-trimethylsilylazacycloalkan-2-ones with alkali metal alcoholate or alkali metal oxide and then alkylation of the alkali metal salts which are formed.
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公开(公告)号:DE2457464A1
公开(公告)日:1976-06-10
申请号:DE2457464
申请日:1974-12-05
Applicant: HOECHST AG
Inventor: SCHORR MANFRED DIPL CHEM DR , SCHRINNER ELMAR DR , SCHMITT WILFRIED
IPC: C07D499/00 , C07D499/46 , C07D499/64 , C07D499/70
Abstract: Acylaminopenicillanic acids of the general formula in which A represents phenyl which may be substituted, an aromatic monocyclic heterocycle which may be substituted or dihydrophenyl, and X represents one of the groups -SO2-, -CO-, -P(R)- or -P(O)(R)- in which R represents low molecular weight alkyl, alkenyl, alkoxy, aralkyl, aralkoxy, aryl or aryloxy which may be substituted, non-toxic salts of these compounds and pharmaceutical compositions containing these compounds.
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公开(公告)号:ZA7507771B
公开(公告)日:1976-11-24
申请号:ZA7507771
申请日:1975-12-12
Applicant: HOECHST AG
Inventor: SCHORR MANFRED , MANFRED SCHORR , SCHRINNER ELMAR , ELMAR SCHRINNER , SCHMITT WILFRIED , WILFRIED SCHMITT
IPC: C07D499/66 , C07D499/00 , C07D499/64 , C07D499/68 , C07D499/70 , C07D
CPC classification number: C07D499/00
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公开(公告)号:DE2458973A1
公开(公告)日:1976-06-16
申请号:DE2458973
申请日:1974-12-13
Applicant: HOECHST AG
Inventor: SCHORR MANFRED DIPL CHEM DR , SCHRINNER ELMAR DR , SCHMITT WILFRIED
IPC: C07D499/66 , C07D499/00 , C07D499/64 , C07D499/68 , C07D499/70
Abstract: Acylaminopenicillanic acids of the general formula in which R1, R2 and R3 represent hydrogen or lower alkyl which may be substituted, and in which the radicals R1 and R2 or R2 and R3 may form together an alkylene radical which may be substituted, R4 and R5 represent hydrogen or lower alkyl, R6 represents phenyl which may be substituted, a monocyclic aromatic heterocycle which may be substituted, or dihydrophenyl, A represents a benzene or thiophene ring which may be substituted, and X represents oxygen or a single bond, a process for preparing them and pharmaceutical compositions active against bacterial infections containing these compounds.
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公开(公告)号:FI753496A
公开(公告)日:1976-06-14
申请号:FI753496
申请日:1975-12-11
Applicant: HOECHST AG
Inventor: SCHORR MANFRED , SCHRINNER ELMAR , SCHMITT WILFRIED
IPC: C07D499/66 , C07D499/00 , C07D499/64 , C07D499/68 , C07D499/70 , C07D
Abstract: Acylaminopenicillanic acids of the general formula in which R1, R2 and R3 represent hydrogen or lower alkyl which may be substituted, and in which the radicals R1 and R2 or R2 and R3 may form together an alkylene radical which may be substituted, R4 and R5 represent hydrogen or lower alkyl, R6 represents phenyl which may be substituted, a monocyclic aromatic heterocycle which may be substituted, or dihydrophenyl, A represents a benzene or thiophene ring which may be substituted, and X represents oxygen or a single bond, a process for preparing them and pharmaceutical compositions active against bacterial infections containing these compounds.
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公开(公告)号:ZA757771B
公开(公告)日:1976-11-24
申请号:ZA757771
申请日:1975-12-12
Applicant: HOECHST AG
Inventor: SCHORR MANFRED , MANFRED SCHORR , SCHRINNER ELMAR , ELMAR SCHRINNER , SCHMITT WILFRIED , WILFRIED SCHMITT
IPC: C07D499/66 , C07D499/00 , C07D499/64 , C07D499/68 , C07D499/70 , C07D
Abstract: Acylaminopenicillanic acids of the general formula in which R1, R2 and R3 represent hydrogen or lower alkyl which may be substituted, and in which the radicals R1 and R2 or R2 and R3 may form together an alkylene radical which may be substituted, R4 and R5 represent hydrogen or lower alkyl, R6 represents phenyl which may be substituted, a monocyclic aromatic heterocycle which may be substituted, or dihydrophenyl, A represents a benzene or thiophene ring which may be substituted, and X represents oxygen or a single bond, a process for preparing them and pharmaceutical compositions active against bacterial infections containing these compounds.
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