104145-95-1Relevant articles and documents
Preparation method of cefditoren pivoxil
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, (2019/02/27)
The invention relates to a preparation method of cefditoren pivoxil. The preparation method comprises the following steps: 7-aminocephalosporanic acid(ACA) is taken as a starting material and subjected to a series of reactions such as iodination and the like after silylation protection to generate parent nucleus for cefditoren, namely 7-amino-3-[(Z)-2-(4-methyl-5-thiazolyl)ethenyl]-3-cephem-4-carboxylic acid (7-ATCA); the compound 7-ATCA firstly reacts with sodium iso-octoate to form sodium salt and then reacts with ethyl 2-(2-aminothiazole-4-yl)-2-methoxyiminoacetate to generate a compound 2,namely cefditoren sodium, under the catalysis of immobilized penicillin acylase; and then the cefditoren sodium reacts with iodomethyl pivalate to obtain a target product, namely cefditoren pivoxil.The preparation method is mild in reaction conditions, environmentally-friendly, high in conversion rate, simple in process, high in content of cis isomers, easy to enlarge and suitable for industrialproduction.
Method for preparing cefditoren pivoxil cephalosporins
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Paragraph 0020; 0031, (2016/10/17)
The invention discloses a method for preparing cefditoren pivoxil cephalosporins.The method comprises the following steps that 1, on the presence of TMEDA and sodium phosphate, 7-ATCA and MAEM are subjected to a contact reaction in THF, and a mixture containing cefditore is obtained, and the contact reaction temperature ranges from 0 to 25 DEG C; 2, the temperature is kept, TEA is added to the mixture containing cefditore obtained in the step 1, then iodomethyl pivalate is added to the mixture to be stirred for reacting, the product is poured into water after the reaction is finished, a saturated ammonium chloride solution is added, the pH is adjusted to be 5 to 5.3, filtering is carried out, and a filter cake obtained through filtering is recrystallized in methyl alcohol to obtain cefditoren pivoxil cephalosporins.According to the method, separation treatment is not needed in the intermediate steps, one-pot operation is easy, cost is reduced, the yield is high, the number of by-products is small, aftertreatment is easy, and the method is especially suitable for industrial popularization.
Process for the preparation of cefditoren using the thioester of thiazolylacetic acid
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Page 2, (2010/02/05)
The present invention provides a process for the preparation of Cefditoren of formula (I) which comprises acylating 7-amino-cephem carboxylic acids of the general formula (IV), where R3 is hydrogen or trimethylsilyl with thioester derivatives of the formula (II), where R1 represents C1-C4 alkyl or phenyl in an organic solvent in the presence of an organic base at a temperature in the range of ?10 ° C. to 30 ° C.