Abstract: Penicillanic acid 1,1-dioxide, and esters thereof readily hydrolyzable in vivo, are useful as antibacterial agents, and also for enhancing the effectiveness of several .beta.-lactam antibiotics against many .beta.-lactamase producing bacteria. Derivatives of penicillanic acid 1,1-dioxide having the carboxy group protected by a conventional penicillin carboxy protecting group are useful intermediates to penicillanic acid 1,1-dioxide. Penicillanic acid 1-oxides and certain esters thereof are useful chemical intermediates to penicillanic acid 1,1-dioxide and its esters.

Abstract: Certain novel 6-acylamino-2,2-dimethyl-3-(5-tetrazolyl)penam derivatives, and salts thereof; their use as broad-spectrum antibacterial agents; and methods for their preparation. Their preparation comprises acylation of the novel intermediate, 6-amino-2,2-dimethyl-3-(5-tetrazolyl)penam or simple derivatives thereof, followed, in some cases, by further transformations of the 6-acylamino group or by removal of a protecting group from the 5-tetrazolyl moiety. Process for the preparation of 6-amino-2,2-dimethyl-3-(5-tetrazolyl)penam, simple derivatives thereof and intermediates therefor.

Abstract: Certain novel 6-acylamino-2,2-dimethyl-3-(5-tetrazolyl)penam derivatives, and salts thereof; their use as broad-spectrum antibacterial agents; and methods for their preparation. Their preparation comprises acylation of the novel intermediate, 6-amino-2,2-dimethyl-3-(5-tetrazolyl)penam or simple derivatives thereof, followed, in some cases, by further transformations of the 6-acylamino group or by removal of a protecting group from the 5-tetrazolyl moiety. Process for the preparation of 6-amino-2,2-dimethyl-3-(5-tetrazolyl)penam, simple derivatives thereof and intermediates therefor.

Abstract: Certain novel antibacterial 7-acylamino-3-substituted-4-(tetrazol-5-yl)-.DELTA..sup.3 -cephem derivatives, and salts thereof, and intermediates useful in their preparation.

Abstract: Certain novel antibacterial 7-acylamino-3-substituted-4-(tetrazol-5-yl)-.DELTA..sup.3 -cephem derivatives, and salts thereof, and intermediates useful in their preparation.

Abstract: Certain novel 6-acylamino-2,2-dimethyl-3-(5-tetrazolyl)penam derivatives, and salts thereof; their use as broad-spectrum antibacterial agents; and methods for their preparation. Their preparation comprises acylation of the novel intermediate, 6-amino-2,2-dimethyl-3-(5-tetrazolyl)penam or simple derivatives thereof, followed, in some cases, by further transformations of the 6-acylamino group or by removal of a protecting group from the 5-tetrazolyl moiety. Process for the preparation of 6-amino-2,2-dimethyl-3-(5-tetrazolyl)penam, simple derivatives thereof and intermediates therefor.

Abstract: Certain novel antibacterial 7-acylamino-3-substituted-4-(tetrazol-5-yl)-.DELTA..sup.3 -cephem derivatives, and salts thereof, and intermediates useful in their preparation.

Abstract: Certain novel antibacterial 7-acylamino-3-substituted-4-(tetrazol-5-yl)-.DELTA..sup.3 -cephem derivatives, and salts thereof, and intermediates useful in their preparation.

Abstract: Certain novel antibacterial 7-acylamino-3-substituted-4-(tetrazol-5-yl)-.DELTA..sup.3 -cephem derivatives, and salts thereof, and intermediates useful in their preparation.

Abstract: The present invention discloses novel 6-acylamino-2,2-dimethyl-3-phosphonopenams and certain lower alkyl esters thereof possessing antibacterial activity, methods for their production, and intermediates therefor; the production comprises the steps of reacting 6-triphenylmethylamino-2,2-dimethylpenam-3-carboxylic acid with lead tetraacetate to form the corresponding 3-acetoxy compound, the latter is converted to .alpha.-triphenylmethylamino-5,5-dimethyl-3-thiazoline-2-acetic acid which is condensed with dimethyl phosphite to produce .alpha.-triphenylmethylamino-5,5-dimethyl-4(0,0-dimethylphosphono)-thiazol idine-2-acetic acid which is cyclized to 6-triphenylmethylamino-2,2-dimethyl-3-(0,0-dimethylphosphono)penam and the latter is subsequently deblocked and acylated.

Abstract: Certain novel antibacterial 7-acylamino-3-substituted-4-(tetrazol-5-yl)-.DELTA..sup.3 -cephem derivatives, and salts thereof, and intermediates useful in their preparation.

Abstract: Certain novel antibacterial 7-acylamino-3-substituted-4-(tetrazol-5-yl)-.DELTA. .sup.3 -cephem derivatives, and salts thereof, and intermediates useful in their preparation.

Abstract: Certain novel antibacterial 7-acylamino-3-substituted-4-(tetrazol-5-yl)-.DELTA..sup.3 -cephem derivatives, and salts thereof, and intermediates useful in their preparation.

Abstract: Certain novel antibacterial 7-acylamino-3-substituted-4-(tetrazol-5-yl)-.DELTA..sup.3 -cephem derivatives, and salts thereof, and intermediates useful in their preparation.

Abstract: The present invention discloses novel 6-acylamino-2,2-dimethyl-3-phosphonopenams and certain lower alkyl esters thereof possessing antibacterial activity, methods for their production, and intermediates therefor; the production comprises the steps of reacting 6-triphenylmethylamino-2,2-dimethylpenam-3-carboxylic acid with lead tetraacetate to form the corresponding 3-acetoxy compound, the latter is converted to .alpha.-triphenylmethylamino-5,5-dimethyl-3-thiazoline-2-acetic acid which is condensed with dimethyl phosphite to produce .alpha.-triphenylmethylamino-5,5-dimethyl-4(0,0-dimethylphosphono)-thiazol idine-2-acetic acid which is cyclized to 6-triphenylmethylamino-2,2-dimethyl-3-(0,0-dimethylphosphono)penam and the latter is subsequently deblocked and acylated.

Abstract: The present invention discloses novel 6-acylamino-2,2-dimethyl-3-phosphonopenams and certain lower alkyl esters thereof possessing antibacterial activity, methods for their production, and intermediates therefor; the production comprises the steps of reacting 6-triphenylmethylamino-2,2-dimethylpenam-3-carboxylic acid with lead tetraacetate to form the corresponding 3-acetoxy compound, the latter is converted to .alpha.-triphenylmethylamino-5,5-dimethyl-3-thiazoline-2-acetic acid which is condensed with dimethyl phosphite to produce .alpha.-triphenylmethylamino-5,5-dimethyl-4(0,0-dimethylphosphono)-thiazol idine-2-acetic acid which is cyclized to 6-triphenylmethylamino-2,2-dimethyl-3-(0,0-dimethylphosphono)penam and the latter is subsequently deblocked and acylated.

Abstract: 6-(D-2-[4-Hydroxy-1,5-naphthyridine-3-carboxamido]-2-[4-hydroxyphenyl]aceta mido-2,2-dimethyl-3-(5-tetrazolyl)penam and the salts thereof are valuable antibacterial agents, particularly for the control of bacterial infections in mammals, especially man.

Abstract: A novel process is described for the preparation of 6-chloro-2-chloromethyl-4-phenylquinazoline-3-oxide, a key intermediate in the synthesis of the known useful psychotherapeutic agents: chlorodiazepoxide and diazepam. This intermediate is prepared by the cyclization of 2-(1'-chloroimino-2'-chloromethyl)-5-chlorobenzophenone, itself a new compound. This compound in turn is prepared by the chloroacetylation of 2-amino-5-chlorobenzophenone to 2-chloroacetamido-5-chlorobenzophenone, another novel compound, and subsequent iminochloride formation.

Abstract: Disclosed herein is an improved process for the preparation of known hypoglycemic piperidinesulfamylureas of the structue ##SPC1##Wherein R is selected from the group consisting of 3-(2-methoxy)pyridyl, 3-(2-ethoxy)pyridyl and 2-(4-chloro)pyridyl and R' is selected from the group consisting of bicyclo[2.2.1]hept-5-en-2-yl-endo-methyl, bicyclo[2.2.1]hept-2-yl-endo-methyl, 7-oxabicyclo[2.2.1]hept-2-yl-methyl, 1-adamantyl and cycloalkyl having from five to eight carbon atoms.Said process comprises contacting 4-(2-pyridyl-amidoethyl) piperidine of the structue ##SPC2##With substantially one equivalent of sulfamide thereby exclusively sulfonating the piperidine nitrogen atom.

Abstract: 5-Carboxypyrimidine derivatives and their pharmaceutically acceptable basic salts, and their use as antiallergy agents.