摘要
(3aS,4S,6aR)-1,3-二苄基-6-(3-甲氧基丙基)四氢噻吩并[3,4-d]咪唑-2-酮在甲酸中和浓盐酸反应制得(3aR,8aS,8bS)-1,3-二苄基-2-氧代十氢咪唑并[4,5-c]噻吩并[1,2-a]氯化锍鎓盐,再经缩合开环、水解后脱羧得到(+)-生物素,总收率73%。
(+)-Biotin was synthesized from (3aS,4S,6aR)-1,3-dibenzyl-6-(3-methoxypropyl)- tetrahydrothieno [3,4-d] imidazol-2-one by chlorination with concentrated hydrochloride to give (3aR,8aS,8bS)-1,3- dibenzyl-2-oxodecahydroimadazo [4,5-c] thieno E 1,2-a] thiolium chloride, which was subjected to condensation and ring opening, hydrolysis and decarboxylation with an overall yield of about 73 %.
出处
《中国医药工业杂志》
CAS
CSCD
北大核心
2009年第3期168-169,共2页
Chinese Journal of Pharmaceuticals
基金
国家级火炬计划项目(2003EB020664)
国家重点新产品(2004ED700014)