38 results about "Cefcapene pivoxil hydrochloride" patented technology

The invention relates to a cefcapene pivoxil hydrochloride composition and a preparation method thereof. The composition consists of a tablet core and a coating layer, wherein the tablet core contains cefcapene pivoxil hydrochloride, a filler, a disintegrating agent, an antisticking agent and a lubricating agent; the grain diameter of the cefcapene pivoxil hydrochloride serving as a raw material is less than 100 micrometers; and the antisticking agent is in an amount which is 3 to 15 percent of the weight of the tablet core. The prepared cefcapene pivoxil hydrochloride tablets have excellent disintegrative property and dissolution of over 75 percent.

The invention relates to a method for preparing cefcapene pivoxil hydrochloride shown as a formula (I). By the method, the reaction time is shortened, the yield is improved, and the safety is high, so that the method is suitable for industrial production.

The invention relates to a cefcapene pivoxil hydrochloride composition and a preparation method thereof. The composition comprises a tablet core and a coating layer, wherein the tablet core comprises cefcapene pivoxil hydrochloride, a filler, a disintegrating agent, an antisticking agent and a lubricating agent; the particle size of the raw material of cefcapene pivoxil hydrochloride is smaller than 100 microns; the antisticking agent accounts for 2%-10% in percentage by weight of the tablet core; the filter comprises a filler such as starch and the like and soluble auxiliary materials; and the soluble auxiliary materials accounts for 1%-10% in percentage by weight of the tablet core. The prepared cefcapene pivoxil hydrochloride tablet has good disintegration, and the dissolution of the cefcapene pivoxil hydrochloride tablet reaches over 75%.

The invention discloses a preparation method for cefcapene pivoxil hydrochloride. The method comprises the following steps: (1) stirring and dissolving a compound which is shown as formula (I) in pyridine, adding methylsufonyl chloride to react to obtain a liquid which contains the compound shown as formula (II), placing the liquid at -15 DEG C to 0 DEG C for later use; (2) in the existence of proline and diisopropylamine, enabling 7-HACA and the liquid which contains the compound shown as the formula (II) to react in methyl alcohol to obtain the compound which is shown as formula (III); (3) adding diisopropylamine, enabling the compound which is shown as the formula (III) and chlorosulfonyl isocyanate to react, regulating the pH to 4 to 5, cooling the organic phase, and adding the diisopropylamine to obtain the compound which is shown as formula (IV); (4) in the existence of potassium phosphate and copper acetate, enabling the compound which is shown as the formula (IV) and iodomethyl pivalate to react in DMF (Dimethyl Formamide) to obtain the compound which is shown as formula (V); (5) removing protecting groups from the compound which is shown as the formula (V) in the methanol solution of hydrochloric acid to obtain the cefcapene pivoxil hydrochloride. According to the method, the product yield is greatly improved, and the method is suitable for industrial production.

The invention relates to a cefcapene pivoxil hydrochloride composition and a preparation method thereof. The composition consists of a tablet core and a coating layer, wherein the tablet core contains cefcapene pivoxil hydrochloride, a filler, a disintegrating agent and a lubricating agent; the grain diameter of the cefcapene pivoxil hydrochloride serving as a raw material is less than 100 micrometers; and the filler consists of a starch filler and soluble auxiliary materials, and the soluble auxiliary materials are in an amount which is 3 to 15 percent of the weight of the tablet core. The prepared cefcapene pivoxil hydrochloride tablets have excellent disintegrative property and dissolution of over 75 percent.

The invention belongs to the technical field of antibiotic drug synthesis, in particular to a synthesis methodof cefcapene pivoxil hydrochloride. The invention is mainly used for process improvement and optimization of cefcapene pivoxil, and the advantage of the synthesis process of cefcapene pivoxil are obvious; new catalytic agents are used, such as phenol, boric acid and other reagents, thereby improving the product quality, increasing the yield, simplifying the operating steps and realizing greater productivity effect and social effect.

The invention provides a preparation method of cefcapene pivoxil hydrochloride intermediate BCN, and belongs to the technical field of organic synthesis. Mixed anhydride BAPA prepared by a mixed anhydride preparation reaction and D-7-ACA-MG salt can be subjected to a condensation reaction, and the cefcapene pivoxil hydrochloride intermediate BCN is obtained by carbamoylation reaction and salt formation crystallization. The preparation method has short process route, high product purity and low cost, and is suitable for industrial production. Data of the embodiment shows that the prepared cefcapene pivoxil hydrochloride intermediate BCN can have purity as high as 98.84% and yield as high as 91.99%.

The invention discloses a synthetic method of cefcapene pivoxil hydrochloride. The synthetic method comprises following steps: 7-aminocephalosporanic acid (7-ACA) is taken as a raw material, and is subjected to 'one-pot reaction' so as to realize 3-esterolysis, and 7-amino protection is carried out; an obtained product is subjected to 'one-pot reaction' so as to realize 3-amidation, and 7-deprotection is carried so as to obtain an important intermediate of cefcapene pivoxil; the intermediate and a derivative of cefcapene pivoxil with an acid side chain are subjected to condensation, and an obtained cefcapene pivoxil precursor with a 4-acid group is subjected to esterification and acidification so as to obtain cefcapene pivoxil hydrochloride finished products. According to the synthetic method, 'atom economy' principle is fully used so as to shorten reaction route, and increase reaction total yield; and it is beneficial for synthetic technology improvement and optimization of cefcapene pivoxil hydrochloride.

The invention discloses a preparation method of cefcapene pivoxil hydrochloride. The preparation method comprises the following steps: 1), a compound shown in the formula I is stirred and dissolved in pyridine, methanesulfonyl chloride is added and stirred for reaction, filtering is performed, and a liquid containing a compound shown in the formula II is obtained; 2), 7-ACA reacts with the liquid containing the compound shown in the formula II in the presence of proline and diisopropylamine, and a compound shown in the formula III is obtained; 3), the compound shown in the formula III reacts with potassium carbonate, and a compound shown in the formula IV is obtained; 4), the compound shown in the formula IV reacts with chlorosulfonyl isocyanate in the presence of diisopropylamine, and a compound shown in the formula V is obtained; 5), the compound shown in the formula V and obtained in the step 4) reacts with iodomethyl pivalate in DMF (dimethyl formamide) in the presence of potassium phosphate and copper acetate, a phosphate solution is added to end the reaction, and a compound shown in the formula VI is obtained; 6), cefcapene pivoxil hydrochloride is obtained after deprotection of the compound shown in the formula VI. The method increases product yield greatly and is particularly suitable for mass production, and few by-products are produced.