摘要
雷美替胺的合成优化是从小分子化合物1，2，6，7-四氢-8H-茚并【5，4-b】呋喃-8-酮中的酮羰基转变为乙氰基，然后乙氰基和与其相连的双键还原，得到2-（1，2，6，7-四氢-8H-茚并[5，4-b】呋喃-8-基）乙胺盐酸盐，对其进行手性拆分，将得到的S-构型异构体与丙酰氯反应得到具有光学活性的雷美替胺：
The improved synthesis of ramelteon was started from 1,2,6,7-tetrahydro-SH-indeno [5,4-b]furan-8-one, whose ketone group was changed to acetonitrile group; then the acetonitrile group and the linked double bond were reduced to 2-（1,2,6,7-tetrahydro-SH-indeno [5,4-b]furan-8-yl）ethylamine hydrochloride salt; the resolving agent is used to chirally resolve the obtained amine to obtain the S-configuration chiral compound, which is reacted with propionyl choloride to form the target compound.
出处
《中国化工贸易》
2012年第7期12-13,16,共3页
CHINA CHEMICAL TRADE
关键词
雷美替胺
拆分
拆分剂
ramelteon
resovle
resolving agenct
