氟苯尼考的制备

Preparation of Florfenicol

在现有的几十条合成路线中,只有以甲砜霉素及其中间体、副产物的合成路线有工业化价值.选用四种路线进行合成试验,结果以D-（-）-苏式-[对-（甲砜基）苯基]丝氨酸乙酯、二氯乙腈为主要原料,经硼氢化钾还原、在催化剂的存在下用二氯乙腈环合、Ishikawa试剂氟化、水解制备氟苯尼考,其收率高于文献值 6%～14%,不生成噁唑啉,实现了绿色合成,避免了臭气的发生,有力地保护了环境,经氟化、水解可直接制备氟苯尼考,无须再与二氯乙酸甲酯反应.由于形成了大规模生产,二氯乙腈价格显著下降,生产成本明显低于其他几种路线.

Formate it in the route in dozens of existing, only the synthetic routes with thiamphnicol,intermediate, by-products have industrialized value. Four kinds of routes are selected in trial-production. The results show that, with D-p-methylsulfino phenyl ethyl serinate as one of the main raw materials, reduced by potassium borohydride, shut with dichoroacetonitrile cyclization under the existence of catalyst, Ishikawa reagent fluorination, hydrolysis the process which prepares florfenicol, could yield 6% - 14% higher than that in the literature, and no malodorous oxazoline is produced. Florfenicol can be produced directly by fluorination and hydrolysis, and no methyl dichloroacetate The praduction cost is lowed with the large scale production.