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以(R)-1-苯乙胺为起始原料,合成了手性氨甲酰基硅烷4。通过4与无手性的亚胺5a、5b和5c以及有手性的亚胺7a、7b和7c反应,得到了立体选择性加成产物α-氨基酰胺衍生物6b、6c、8a、8b和8c,其中6c、8a和8c是高立体选择性产物。手性氨甲酰基硅烷与亚胺的反应具有立体选择性,其立体选择性大小与在亚胺双键氮原子和碳原子上所连的取代基有关,因此通过选择不同的取代基可有效地不对称合成α-氨基酰胺衍生物。
Starting from (R) -1-phenylethylamine, chiral carbamoylsilane 4 was synthesized. The stereoselective addition products α-aminoamide derivatives 6b, 6c, 8a, 8b and 6c are obtained by reaction of 4 with achiral imines 5a, 5b and 5c and the chiral imines 7a, 7b and 7c 8c, where 6c, 8a and 8c are highly stereoselective products. The reaction of chiral carbamylsilanes with imines is stereoselective in that their stereoselectivity is related to the number of substituents attached to the nitrogen and the carbon atoms of the imine double bond so that by choosing different substituents it is effective Asymmetric Synthesis of α-Aminoamide Derivatives.