Graduate School of Pharmaceutical Sciences, Kyushu University, CREST, Maidaashi Higashi-ku, Fukuoka, 812-8582, Japan.
Chemistry. 2013 Jun 24;19(26):8417-20. doi: 10.1002/chem.201301237. Epub 2013 May 13.
A green way to amino acids: α-Tetrasubstituted α-amino acid derivatives are formed in high yield and enantioselectivity by using a Rh-catalyzed enantioselective alkynylation of α-ketiminoesters. This reaction, which involves a proton transfer and can be conducted at room temperature, has high substrate scope (see scheme; Cbz = benzyloxycarbonyl, Fmoc = 9-fluorenylmethyloxycarbonyl).
通过 Rh 催化的α-酮亚胺酯的对映选择性炔基化反应,可以高产率和对映选择性地得到α-四取代α-氨基酸衍生物。该反应涉及质子转移,可在室温下进行,具有广泛的底物范围(见方案;Cbz = 苄氧羰基,Fmoc = 9-芴甲氧羰基)。