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受广西区科委的委托,南宁市科委于1987年12月28日在南宁召开了省级技术鉴定会,南宁制药二厂承担的全合成延胡索乙素工业性生产试验科研项目通过鉴定。延胡索乙素(即四氢巴马汀外消旋体),系临床上广为应用的镇痛药。过去,一直以野生植物黄藤中的巴马汀为原料,半合成生产。由于植物资源贫乏,产品供不应求。近年来南宁制药二厂采用愈刨木酚为原料,经甲基化、氯甲基化氰化、胺化、缩合还原、环合、氢化精制等化学反应,全合成延胡索乙素获得成功,工业性生产试验收率达14.36%。以愈创木酚为原料全合成延胡索乙素工业性生产试验,为国内首创。经专家审议,认为该工艺路线切实可行,收率比较稳定,质量达到广西药品标准,“三废”治理可达到国家排放标准。
Entrusted by the Guangxi Science and Technology Commission, the Nanning Science and Technology Commission held a provincial-level technical appraisal meeting in Nanning on December 28, 1987. The fully synthetic tetrahydropalmatine industrial production test and research project undertaken by Nanning Pharmaceutical Plant No. 2 passed the appraisal. Tetrahydropalmatine, the racemate of tetrahydropalmatine, is an analgesic widely used clinically. In the past, palmatine was used as a raw material and was semi-synthesized. Due to the lack of plant resources, the supply of products is in short supply. In recent years, Nanning Pharmaceutical Factory No. 2 used the plant wood as the raw material, and methylation, chloromethylation, cyanation, amination, condensation reduction, cyclization, and hydrorefining were the chemical reactions. The total synthesis of tetrahydropalmatine was successful. The test yield of sexual production reached 14.36%. The industrial production test of tetrahydropalmatine was synthesized using guaiacol as raw material, which was the first in China. After deliberation by experts, it is believed that the process route is feasible, the yield is relatively stable, the quality has reached the Guangxi drug standards, and the “three wastes” treatment can meet the national emission standards.