摘要:
Cefamandole is produced by the consecutive steps of A. MIXING SUBSTANTIALLY EQUIMOLAR WEIGHTS OF PHOSPHONITRILIC CHLORIDE TRIMER AND OF A DERIVATIVE OF D-mandelic acid having the formula
OR A SALT THEREOF AND C. REMOVING SAID HYDROXYL BLOCKING GROUP R by conventional chemical methods to produce said cefamandole or salt thereof.
WHEREIN THE HYDROXYL BLOCKING GROUP R represents dichloroacetyl, silyl, tetrahydropyranyl or formyl in an organic solvent; B. ADDING THERETO, PREFERABLY SLOWLY, A SOLUTION CONTAINING SUBSTANTIALLY THE SAME NUMBER OF MOLES OF 7-AMINO-3-(1METHYLTETRAZOL-5-YL)THIOMETHYL-3-CEPHEM-4-CARBOXYLIC ACID OR A SALT OR AN EASILY HYDROLYZED Schiff base thereof to produce the intermediate acid having the formula
摘要:
7-(D-( Alpha -Amino- Alpha -phenyl-, 2-thienyl- and 3thienylacetamido)-3-(3-methyl-1,2,5-oxadiazol-4yl)carbonylthiomethyl-3 -cephem-4-carboxylic acids and their pharmaceutically acceptable salts are valuable as antibacterial agents, as nutritional supplements in animal feeds, as agents for the treatment of mastitis in cattle and as therapeutic agents in poultry and animals, including man. The compounds are especially useful in the treatment, particularly by oral administration, of infectious diseases caused by many Gram-positive and Gramnegative bacteria. Also included within the invention are easily cleavable esters of the abovementioned acids and pharmaceutically acceptable acid addition salts of said esters.
摘要:
Cefamandole is produced by the consecutive steps of A. MIXING SUBSTANTIALLY EQUIMOLAR WEIGHTS OF N-ethoxycarbonyl-2ethoxy-1,2-dihydroquinoline and of a derivative of D-mandelic acid having the formula
WHEREIN THE HYDROXYL BLOCKING GROUP R represents dichloroacetyl, silyl, tetrahydropyranyl or formyl is an organic solvent; B. ADDING THERETO, PREFERABLY SLOWLY, A SOLUTION CONTAINING SUBSTANTIALLY THE SAME NUMBER OF MOLES OF 7-AMINO-3-(1METHYLTETRAZOL-5-YL)THIOMETHYL-3-CEPHEM-4-CARBOXYLIC ACID OR A SALT OR AN EASILY HYDROLYZED Schiff base thereof to produce the intermediate acid having the formula
OR A SALT THEREOF AND C. REMOVING SAID HYDROXYL BLOCKING GROUP R by conventional chemical methods to produce said cefamandole or salt thereof.
摘要:
THE SPECIFICATION DISCLOSES THE COMPOUND PIVALOYLOXYMETHYL HETACILLINATE AND A METHOD FOR THE PREPARATION THEREOF. THIS COMPOUND IS USEFUL IN THE TREATMENT OF INFECTIOUS DISEASES IN MAMMALS.
摘要:
PIVALOYLOXYMETHYL 6 - (D -A - SULFOAMINOPHENYLACETAMIDO) PENICILLANATE SODIUM SALT (I) IS A VALUABLE ANTIBIOTIC AGENT, NUTRITIONAL SUPPLEMENT IN ANIMAL FEED, THERAPEUTIC AGENT IN POULTRY AND ANIMALS, INCLUDING MAN, AND IS ESPECIALLY USEFUL IN THE TREATMENT OF INFECTIOUS DISEASES CAUSED BY GRAM-POSITIVE AND GRAM-NEGATIVE BACTERIA, MOST PARTICULARLY THOSE CAUSED BY THE PSEUDOMONAS GENUS, SODIUM PIVALOYLOXYMETHYL 6-(D-A-SULFOAMINOPHENYLACETAMIDO)PENICILLANATE IS PREPARED BY THE TREATMENT OF DISODIUM 6-(D-A-SULFOAMINOPHENYLACETAMIDO) PENICILLANATE (II) WITH CHLOROMETHYL PIVALATE IN HEXAMETHYLPHOSPHORTRIAMIDE. COMPOUND I HAS A SIMILAR ANTIBACTERIAL SPECTRUM TO THAT OF COMPOUND II BUT IS ABSORBED FROM THE GASTRO-INTESTINAL TRACT 2-3 FOLD MARE EFFICIENTLY THAN COMPOUND II.