(R)-1-苯基-1,2,3,4-四氢异喹啉的转化利用

以(R)-1-苯基-1,2,3,4-四氢异喹啉为原料,在18-冠-6存在下,KMnO4选择性的氧化为1-苯基-3,4-二氢异喹啉,再经KBH4的还原生成1-苯基-1,2,3,4-四氢异喹啉,D-酒石酸拆分,最终得到索菲那新的中间体(S)-1-苯基-1,2,3,4-四氢异喹啉,反应总产率32.2%,目标产物结构经熔点检测和1HNMR表征;重点研究了选择性氧化的影响因素,确定了最优反应条件。该工艺有效利用了(R)-1-苯基-1,2,3,4-四氢异喹啉,节约了成本,具有一定的经济价值。

Conversion and Utilization of (R)-1-phenyl-1,2,3,4-tetrahydro-isoquinoline

he (R)-1-phenyl-1,2,3,4-tetrahyro-isoquinonine was used as the starting material to synthesis the intermediate of Solifenacin, (S)-1-phenyl-1,2,3,4-tetrahydro-isoquinoline,by tree steps : Selective Oxidation with KMnO4 in the presence of 18-Crown-6, Reduction with KBH4,Resolution with D-tartaric acid. The total yield is 32.2%. The structure of target product was identified by Melting point determination and 1HNMR spectroscopy. The study was focused on the selective oxidation of factors and the optimal conditions were obtained.The craft made used of the (R)-1-phenyl-1,2,3,4-tetrahydro-isoquinonine effectively and saved the cost, which has some economic value.