Dalian Institute of Chemical Physics, Chinese Academy of Sciences, Dalian 116023, China.
J Org Chem. 2010 Dec 3;75(23):8319-21. doi: 10.1021/jo101849b. Epub 2010 Nov 9.
A series of chiral 3-aryl-4-phosphonobutyric acid esters were synthesized in high enantioselectivities (93-98% ee) via the Rh-catalyzed asymmetric hydrogenation of the corresponding 3-aryl-4-phosphonobutenoates using a P-stereogenic BoPhoz-type phosphine-aminophosphine ligand. The methodology has been successfully applied to the asymmetric synthesis of a potential GABA(B) antagonist, (R)-phaclofen, in high enantioselectivity.
通过使用手性 BoPhoz 型膦-氨基膦配体，铑催化的相应 3-芳基-4-膦烯丁酸酯的不对称氢化反应，以高对映选择性（93-98%ee）合成了一系列手性 3-芳基-4-膦丁二酸酯。该方法已成功应用于潜在 GABA(B)拮抗剂（R）-phaclofen 的高对映选择性不对称合成。
