The present invention relates to a process for the efficient preparation of enantiomerically enriched beta amino acid derivatives wherein the amino group is unprotected. The product chiral beta amino acid derivatives are useful in the asymmetric synthesis of biologically active molecules. The process comprises an enantioselective hydrogenation of an amine-unprotected prochiral beta-amino acrylic acid or derivative thereof in the presence of a rhodium metal precursor complexed with a chiral mono- or bisphosphine ligand.
本发明涉及一种高效制备非保护
氨基的对映富集的β-
氨基酸衍
生物的方法。该产物手性的β-
氨基酸衍
生物在
生物活性分子的不对称合成中有用。该方法包括在手性单或双
膦配体络合的
铑金属前体存在下,对未保护
氨基的
丙烯酸β-
氨基酸或其衍
生物进行对映选择性的氢化。