论文部分内容阅读
由于(+)-生物素在人类和动物营养中的重要性以及人类和动物对合成维生素需求的日益增长,促进了(+)-生物素的合成研究。近来报道的几种新的合成方法,就工业生产方面而言,与长期使用的Sternbach-Hoffmann-La Roche路线相比,没有明显的优点。这里报道的是一条新的简便的合成路线(见图)。化合物1由L-胱氨酸二甲酯与光气作用转化为双异腈酸酯,然后用苄胺处理而得(两步反应产率均为91％),用3当量的三苯膦(7:2:1的二甲氧基乙烷:甲醇:水混合溶剂,
The (+) - biotin synthesis has been promoted due to the importance of (+) - biotin in human and animal nutrition and the increasing demand for synthetic vitamins in humans and animals. Several new synthetic methods recently reported have no clear advantage in terms of industrial production over the long-running Sternbach-Hoffmann-La Roche route. Here is a new easy synthesis route (see photo). Compound 1 was converted from L-cystine to phlorosponine to bis-isocyanurate and then treated with benzylamine (91% yield for both steps) using 3 equivalents of triphenylphosphine ( Dimethoxyethane: methanol: water mixed solvent of 7: 2: 1,