Industrial production method for clindamycin or salts thereof

A technology of clindamycin and lincomycin, applied in the direction of sugar derivatives, organic chemistry, etc., can solve the problems of low yield, cumbersome operation, HPLC purity rarely reaches 90%, etc. The effect of easy handling and high product purity

Active Publication Date: 2008-12-31
重庆凯林制药有限公司 +1
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Triphenylphosphine is expensive and is converted into triphenylphosphine oxide after the chlorination reaction, which brings difficulties to the subsequent refining of finished products
[0023] But said method has limitations equally: or yield is on the low side or operation is loaded down with trivial details etc., especially when adopting said method to prepare clindamycin hydrochloride, it is often more difficult in aftertreatment and finished product refining stage, therefore makes the HPLC purity of finished product very low less than 90%

Method used

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  • Industrial production method for clindamycin or salts thereof
  • Industrial production method for clindamycin or salts thereof
  • Industrial production method for clindamycin or salts thereof

Examples

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Effect test

Embodiment 1

[0048] 1. Chloride Preparation

[0049] 1.1 Chlorinating agent [(CH 3 ) 2 N=CHCl + ] Cl - preparation of

[0050] At 25±5°C, pump 270kg of chloroform into the reactor, add 115kg of N,N-dimethylformamide, and pump it into the high-level tank. Then add 375 kg of chloroform and 126.5 kg of bis-trichloromethyl carbonate into the main reaction pot, blow nitrogen, and when the ice brine drops to 0°C, start to add the N,N-dimethylformamide prepared above dropwise. Chloroform solution of amide, maintain the internal temperature at 10±2°C during the dropwise addition. After dropping, stir for 1 hour, heat up to an internal temperature of 15-25°C and react for 0-3 hours, cool down in ice-water solution to obtain the chlorinated agent [(CH 3 ) 2 N=CHCl + ] Cl - solution.

[0051] 1.2 Preparation of Chloride

[0052]When the internal temperature dropped below -2°C, 100 kg of lincomycin hydrochloride was added under the protection of nitrogen, and the interlayer was maintained t...

Embodiment 2

[0072] According to the method of embodiment 1, just replace 126.5kg bis-trichloromethyl carbonate with 150kg trichloromethyl chloroformate, obtain clindamycin hydrochloride, HPLC purity 97.8%, total molar yield is calculated with respect to lincomycin hydrochloride 78% to 86%.

Embodiment 3

[0074] According to the method of embodiment 1, just replace 100kg lincomycin hydrochloride with 95kg lincomycin free base, obtain clindamycin hydrochloride, HPLC purity>98%, total molar yield is calculated as to lincomycin free base 80% to 87%.

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Abstract

The invention relates to an industrial production method for producing clindamycin or the salts of clindamycin. The method uses dual-trichloromethyl carbonate or trichloromethyl methyl chloroformate and amide to prepare the intermediate chlorophthalic agent. The method of the invention has high product purity, high yield, easier post-processing and other technical advantages, compared with the prior art.

Description

technical field [0001] The invention relates to a method for industrial production of clindamycin or its salts, in particular to a method for producing clindamycin hydrochloride by using an intermediate chlorination agent prepared by the new method. Background technique [0002] Clindamycin (structure shown below), also known as clincomycin, is an antibiotic obtained semisynthetically from lincomycin (structure shown below). Clindamycin hydrochloride is clinically used to treat infections caused by anaerobic bacteria, staphylococcus, streptococcus, pneumococcus, etc., and its effect is 4 to 8 times stronger than lincomycin hydrochloride. [0003] [0004] Structure of Lincomycin Structure of Clindamycin [0005] The key to the synthesis of clindamycin hydrochloride lies in the selection of the chlorination agent used therein. The key point of the whole process is to select a suitable chlorination agent to replace the hydroxyl group at the 7-position of lincomycin and re...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07H15/16
Inventor 龙道兵韩兆锋郭钱浩周旭东
Owner 重庆凯林制药有限公司
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