PROCESS FOR PREPARING CEPHALOSPORIN SALTS

CRYSTALLINE SULFURIC, DI-NITRIC, MONO-HYDROCHLORIC DI-HYDROCLORIC, AND DI AND SESQUIORTHOSPHOSPHORIC ADDITION SALTS OF 7-<A-(AMINOTHIAZOL-4-YL)-A-(Z)-METHOXYIMINOACETAMIDO>-3-<(1-METHYL-1-PYRROLIDINIO)-METHYL>-3-CEPHEM-4-CARBOXYLATE ARE STABLE EVEN AT ELEVATED TEMPERATURES. THE CRYSTALLI...

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Bibliographic Details
Main Authors LIPPER, ROBERT A, KAPLAN, MURRAY A, HUDYMA, THOMAS W
Format Patent
LanguageEnglish
Korean
Published 19.04.1993
Edition5
Subjects
CHEMISTRY
HETEROCYCLIC COMPOUNDS
HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
METALLURGY
ORGANIC CHEMISTRY
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS
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Summary:CRYSTALLINE SULFURIC, DI-NITRIC, MONO-HYDROCHLORIC DI-HYDROCLORIC, AND DI AND SESQUIORTHOSPHOSPHORIC ADDITION SALTS OF 7-<A-(AMINOTHIAZOL-4-YL)-A-(Z)-METHOXYIMINOACETAMIDO>-3-<(1-METHYL-1-PYRROLIDINIO)-METHYL>-3-CEPHEM-4-CARBOXYLATE ARE STABLE EVEN AT ELEVATED TEMPERATURES. THE CRYSTALLINE SURFURIC ACID ADDITION SALT IS MADE BY FORMING AN ADMIXTURE OF (A) AT LEAST ONE MOLAR EQUIVQLENT OF SULFURICACID WITH (B) ZWITTERION IN AN AMOUNT SO AS TO BE PRESENT IN THE ADMIXTURE AT A CONCENTRATION OF GREATER THAN 25 MILLIGRAMS/ML, CAUSING CRYSTALLIZATION, SEPARATING THE CRYSTALS, WASHINGAND DRYING. THE CRYSTALLINE MONOHYDROCHLORIDE, AND ORTHOPHOSPHATE SALTS ARE PREPARED BY DISSOLVING THE ZWITTERION IN THE APPROPRIATE AMOUNT OF ACID, CAUSING CRYSTALLIZATION BY ADDING ACETONE AND ISOLATING THE CRYSTALS. PHYSICAL ADMIXTURES OF THE SALTS WITH CERTAIN BASES IN PROPORTIONS TO GIVE A PH RANGING FROM ABOUT 3.5 TO ABOUT 7 ON DILUTION WITH WATER PROVIDE INJECTABLE COMPOSITIONS ON DILUTION.
Bibliography:Application Number: KR19860006445