The Institute of Scientific and Industrial Research, Osaka University , 8-1 Mihogaoka, Ibaraki-shi, Osaka 567-0047, Japan.
Graduate School of Pharmaceutical Sciences, Osaka University , 1-6 Yamada-oka, Suita-shi, Osaka 565-0871, Japan.
Org Lett. 2017 Oct 6;19(19):5426-5429. doi: 10.1021/acs.orglett.7b02693. Epub 2017 Sep 28.
The first enantio- and diastereoselective Betti/intramolecular aza-Michael sequence carried out using a C-symmetric chiral trisimidazoline organocatalyst is reported. The reaction of phenols and N-tosylimines bearing a Michael acceptor moiety afforded densely functionalized 1,3-disubstituted isoindolines bearing two stereogenic centers as single diastereomers in high yields (≤93%) and excellent enantioselectivities (≤99.9%).
首次报道了使用 C 对称手性三咪唑啉有机催化剂进行的对映选择性和非对映选择性贝蒂/分子内氮杂迈克尔反应。带有迈克尔受体部分的酚和 N-对甲苯磺酰亚胺的反应以高产率（≤93%）和优异的对映选择性（≤99.9%）得到了两个手性中心的高度官能化的 1,3-二取代异吲哚啉作为单一非对映异构体。
Zotero 插件