2-甲硫基-2-噻唑啉合成工艺研究  

Study on Synthesis of 2-(methylthio)-2-thiazoline

作　　者：毛文华 谢菊冲 陶敏杰 石岳崚 赵晓江 徐丹萍 MAO Wen-hua;XIE Ju-chong;TAO Min-jie;SHI Yue-ling;ZHAO Xiao-jiang;XU Dan-ping(Zhejiang Hisoar Pharmaceutical Co., Ltd., Zhejiang Taizhou 318000, China)

机构地区：[1]浙江海翔药业股份有限公司

出　　处：《广州化工》2019年第15期38-39,共2页GuangZhou Chemical Industry

摘　　要：替比培南酯是目前唯一一个可以口服的碳青霉烯类抗生素,2-甲硫基-2-噻唑啉是替比培南侧链中间体,2-甲硫基-2-噻唑啉质量是影响替比培南侧链关键因素;2-甲硫基-2-噻唑啉合成以2-巯基-2-噻唑啉为起始原料,甲醇为溶剂,碳酸钾作为缚酸剂,选用碘甲烷为经典甲基化试剂;反应温度25~30℃;反应时间4. 5 h最好;收率99%,纯度大于99%;操作简单,适合工业化生产。Tebipenem pivoxil is currently the only oral carbapenem antibiotics. 2-(methylthio)-2-thiazolineisan is the intermediate on the Tebipenem pivoxil side chain. The quality of 2-methyl-2-thiazoline is the key factor affecting the Tebipenem pivoxil side chain. 2-methylthio-2-thiazoline was synthesized by using 2-mercapto-2-thiazoline as the starting material,methanol as solvent,and potassium carbonate as acid binder. The methylene iodide was selected as the classical methylation reagent. The reaction temperature was 25 ~ 30 ℃,the optimum reaction time was 4. 5 h,the yield was 99% and the purity was greater than 99%. This method was simple in operation,and suitable for industrial production.

关 键 词：起始原料 甲基化试剂 2-甲硫基-2-噻唑啉 合成 

分 类 号：TQ46[化学工程—制药化工]