METHOD OF OBTAINING AMINOTHIASOLYL DERIVATIVES OF CEPHALOSPORINE AS WELL AS THEIR SODIUM OR POTASSIUM SALTS
1. Process for producing amino thiazolyl derivatives of cephalosporin and their sodium or potassium salts with general formula 1, where X denotes acetoxyl group, N- pyridyl group substituted or not substituted with alkyl group with 1-6 atoms of carbon, heterocyclic thiole, optimally 2-methyl-5,6-dio...
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Sprache: | eng |
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Zusammenfassung: | 1. Process for producing amino thiazolyl derivatives of cephalosporin and their sodium or potassium salts with general formula 1, where X denotes acetoxyl group, N- pyridyl group substituted or not substituted with alkyl group with 1-6 atoms of carbon, heterocyclic thiole, optimally 2-methyl-5,6-dioxy-1,2,5,6-tetrahydro-1,2,4-triazine-3-thiol or its tautometer, tetrazole thiole or thiazolo thiole group, R denotes methylene or alkane carboxyl group of lower fatty acids with 2-6 atoms of carbon, while R denotes atom of hydrogen, sodium or potassium ammonium group, silyl, alkyl or aryl with 1-20 atoms of carbon, by activating Z,2(2-amino thiazolyl)-2-alcoxy iminoacetic acid and condensation of the produced active form of acid with sodium, potassium or salt of ammonium or silyl, alkyl of aryl ester derivative of 7- aminocephalosporin acid, characterised in that the activation process of Z ,2(2-amino thiazolyl)-2-alcoxy iminoacetic acid is conducted in acetonitrile in temperature from 0 degree C to -40 degrees C using N,N daily chlorosulfite alkane imonium derived from dialkyl amide, optimally dimethylformamide, dimethylacetamide or N-methylpyrrolidone and thionyl chloride in temperature higher than 40 degrees C, and the obtained active form is subject to condensation using known methods by adding to the solution cephalosporin acid derivative, while pH of the mixture is maintained within 5-10. |
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