Tanaka Yuta, Kanai Motomu, Shibasaki Masakatsu
Graduate School of Pharmaceutical Sciences, The University of Tokyo, Hongo, Bunkyo-ku, Tokyo 113-0033, Japan.
J Am Chem Soc. 2008 May 14;130(19):6072-3. doi: 10.1021/ja801201r. Epub 2008 Apr 18.
The first synthetically useful catalytic enantioselective conjugate addition of cyanide to enones is described. The optimized conditions involved a Gd catalyst (5 or 10 mol %) derived from ligands 3 or 4 and a 1:1 ratio of TBSCN and 2,6-dimethylphenol. The reaction exhibited excellent to high enantioselectivity and a wide substrate scope. Moreover, the 1,4-adduct was exclusively produced over the 1,2-adduct. The complete regioselectivity was due both to stabilization of the 1,4-selective silylated polymetallic catalyst (7) using a TBS group and the ability of the asymmetric catalyst to promote retro-cyanation from the 1,2-adduct.
首次描述了用于合成的氰化物对烯酮的催化对映选择性共轭加成反应。优化条件包括由配体3或4衍生的钆催化剂(5或10 mol%)以及TBSCN与2,6-二甲基苯酚1:1的比例。该反应表现出优异至高的对映选择性以及广泛的底物范围。此外,只生成1,4-加合物而非1,2-加合物。完全的区域选择性既归因于使用TBS基团对1,4-选择性硅烷基化多金属催化剂(7)的稳定作用,也归因于不对称催化剂促进1,2-加合物进行逆氰化反应的能力。