Hayashi Yujiro, Sakamoto Daisuke, Okamura Daichi
Department of Chemistry, Graduate School of Science, Tohoku University , 6-3 Aramaki-Aza Aoba-ku, Sendai, Miyagi 980-8578, Japan.
Org Lett. 2016 Jan 4;18(1):4-7. doi: 10.1021/acs.orglett.5b02839. Epub 2015 Dec 4.
An efficient asymmetric total synthesis of (S)-baclofen was accomplished via a one-pot operation from commercially available materials using sequential reactions, such as aldol condensation of acetaldehyde, diphenylprolinol silyl ether mediated asymmetric Michael reaction of nitromethane, Kraus-Pinnick oxidation, and Raney Ni reduction. Highly enantioenriched baclofen was obtained in one pot with a good yield over four reactions.
通过一锅法操作，以市售原料为起始物，利用连续反应，如乙醛的羟醛缩合、二苯基脯氨醇硅醚介导的硝基甲烷不对称迈克尔反应、克劳斯 - 平尼克氧化反应以及阮内镍还原反应，完成了(S)-巴氯芬的高效不对称全合成。通过这四个反应，在一锅法中以良好的产率获得了高对映体富集的巴氯芬。
