Efficient kinetic resolution in the asymmetric hydrosilylation of imines of 3-substituted indanones and 4-substituted tetralones.
Efficient kinetic resolution in the asymmetric hydrosilylation of imines of 3-substituted indanones and 4-substituted tetralones.
复制标题
3-取代茚满酮和 4-取代四氢萘酮亚胺不对称氢化硅烷化的高效动力学拆分。
DOI：
10.1021/jo991328h
复制
发表时间：
2000
期刊：
影响因子：
--
通讯作者：
Buchwald,SL
中科院分区：
文献类型：
--
作者：
Yun,J;Buchwald,SL
在手性茂钛催化剂作用下，可实现3-取代茚满酮和4-取代四氢萘酮的N-甲基亚胺的动力学拆分，其中4-取代四氢萘酮的N-甲基亚胺经水解后可得到高ee值的酮和高非对映体和对映体纯度的胺产物。在舍曲林的合成中证明了该方法的实用性。
Kinetic resolution of theN-methyl imines of 3-substituted indanones and 4-substituted tetralones could be accomplished by hydrosilylation with a chiral titanocene catalyst.N-Methyl imines of 4-substituted tetralones were resolved to yield, after hydrolysis of the unreacted starting materials, ketones with high ee's and the amine products with high diastereomeric and enantiomeric purity. The utility of this process was demonstrated in the synthesis of sertraline.