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filingDate 1974-02-22-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationDate 1976-05-16-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber ES-423531-A1
titleOfInvention A PROCEDURE FOR THE PREPARATION OF ALPHA-AMINOACIL-3- HALO-CEPHALOSPORIN.
abstract A procedure for the preparation of α-aminoacyl 3-halo-cephalosporin of the formula: **(See formula)** where R is phenyl, hydroxyphenyl, halophenyl, methylphenyl, methoxyphenyl, 2-thienyl, 3-thienyl or 2-furyl; R1 is hydrogen, benzyl, p-methoxybenzyl, p-nitrobenzyl, diphenylmethyl, 2,2,2-trichlorethyl, trimethylsilyl or tert-butyl; R2 is hydrogen or tert-butyloxycarbonyl, benzyloxycarbonyl, p-nitrobenzyloxycarbonyl, trichloroethoxycarbonyl or trityl, or enamines formed with methyl acetoacetate and acetylacetone; X is chlorine or bromine; and its non-toxic and pharmaceutically acceptable salts; whose procedure is characterized by: a) reacting a 3-halo-3-cephemic ester of the formula: **(See formula)** where R1 and X are as defined above, with an acylating agent of the formula: **(See formula)** or an active derivative thereof, to give the corresponding 7- (α-amino) or 7- (protected α-amino) acylamido-3-halo-3-cephem-4-carboxylic acid ester and b) optionally removing the carboxylic acid protecting ester forming group or amino protecting group to give the corresponding 7- (α-amino) acylamido-3-halo-3-cephem-4-carboxylic acid. (Machine-translation by Google Translate, not legally binding)
priorityDate 1973-02-23-04:00^^<http://www.w3.org/2001/XMLSchema#date>
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