Kato Naoya, Shirai Tomohiko, Yamamoto Yasunori
Division of Chemical Process Engineering and Frontier Chemistry Center (FCC), Faculty of Engineering, Hokkaido University, Kita 13 Nishi 8 Kita-ku, Sapporo, Hokkaido, 060-8628, Japan.
Chemistry. 2016 Jun 1;22(23):7739-42. doi: 10.1002/chem.201601246. Epub 2016 Apr 27.
Chiral rhodium(I)-catalyzed highly enantioselective arylation of aliphatic N-sulfonyl aldimines with arylboronic acids has been developed. This transformation is achieved by the use of a rhodium/bis(phosphoramidite) catalyst to give enantiomerically enriched α-branched amines (up to 99 % ee). In addition, this system enables efficient synthesis of (+)-NPS R-568 and Cinacalcet which are calcimimetic agents.
已开发出一种手性铑（I）催化的脂肪族N-磺酰基醛亚胺与芳基硼酸的高度对映选择性芳基化反应。通过使用铑/双（磷酰胺）催化剂实现这种转化，得到对映体富集的α-支链胺（对映体过量高达99%）。此外，该体系能够高效合成拟钙剂（+）-NPS R-568和西那卡塞。
