Method for preparing cefotiam hexetil hydrochloride

A technology of cefotiam and cefotiam, which is applied in the field of drug antibiotics and can solve the problems of increasing crystallization loss and increasing separation processes, etc.
CN101948476BInactive Publication Date: 2012-07-25国药集团致君(苏州)制药有限公司
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
国药集团致君(苏州)制药有限公司
Publication Date
2012-07-25
Estimated Expiration
Not applicable · inactive patent

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Abstract

The invention discloses a method for preparing and purifying cefotiam salt and cefotiam hexetil hydrochloride. The method comprises the following steps of: reacting cefotiam with bicarbonate to prepare cefotiam salt; and reacting the prepared and purified 1-iodoethyl cyclohexyl carbonate with the cefotiam salt to prepare the cefotiam hexetil. The cefotiam hexetil hydrochloride is prepared by performing hydrochloric acidification and purification on the cefotiam hexetil. The method for preparing the cefotiam hexetil hydrochloride has a simple preparation process, at the purification part, the extraction is combined with crystallization by using a mixed solvent, and meanwhile, a water-soluble reducing agent is added in a step of easily changing color, so that the finished product of high purity, high yield and good color is obtained. The cefotiam hexetil hydrochloride prepared by the method of the invention has the purity of over 98.5 percent and the yield of over 95 percent.
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Description

technical field

[0001] The invention relates to the preparation of cefotiam axetil, in particular to a method for preparing and purifying cefotiam axetil hydrochloride, which belongs to the field of drug antibiotics. Background technique

[0002] Cefotiam (CTM) is a second-generation cephalosporin, its structural formula is shown in formula (I), cefotiam esterification can obtain cefotiam hexetil (Cefotiam hexetil), its structural formula is shown in formula (II).

[0003]

[0004] Cefotiam can be made into oral antibiotics. The oral antibiotics themselves have no antibacterial effect. After oral administration, they are quickly hydrolyzed into cefotiam in the intestinal mucosa and absorbed. Cefotiam has the same antibacterial activity against Gram-positive and negative bacteria as The cephalosporins orally administered in the past are the same, and they are stable to β-lactamase. They are effective against clinically isolated Staphylococcus aureus, coagulase-negative sta...

Claims

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