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探索不对称合成α-氨基酰胺衍生物的方法。方法以(R)-1-苯乙胺为起始原料,首先合成手性氨甲酰基硅烷,然后,该手性氨甲酰基硅烷分别与非手性亚胺、手性亚胺反应,最终得到立体选择性加成产物α-氨基酰胺衍生物。结果与结论合成了5个α-氨基酰胺衍生物,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亚胺双键氮原子和碳原子上所连的烃基有关,因此通过选择不同的烃基可实现不对称合成α-氨基酰胺衍生物的目的。
To explore asymmetric synthesis of α-aminoamide derivatives method. Methods Starting from (R) -1-phenylethylamine, chiral carbamoylsilane was firstly synthesized, and then the chiral carbamoylsilane reacted with achiral imine and chiral imine respectively to finally obtain Stereoselective Addition Products α-Aminoamide Derivatives. RESULTS AND CONCLUSIONS Five α-aminoamide derivatives were synthesized, among which 6c, 8a and 8c were highly stereoselective products. The reaction between chiral carbamylsilane and imine has the stereoselectivity, the stereoselectivity is related to the nitrogen atom of imine double bond and the hydrocarbon group connected to the carbon atom. Therefore, the asymmetric synthesis of α -amino amide derivatives.