The precise control of Z and E configurations of the carbon-carbon double bond in alkene synthesis has long been a fundamental challenge in synthetic chemistry, even more pronounced when simultaneously striving to achieve enantioselectivity [( Z , R ), ( Z , S ), ( E , R ), ( E , S )]. Moreover, enantiopure non-natural α-amino acids are highly sought after in organic and medicinal chemistry. In this study, we report a ligand-controlled stereodivergent synthesis of non-natural α-quaternary amino acids bearing trisubstituted alkene moieties in high yields with excellent enantioselectivity and Z / E selectivities. This success is achieved through a palladium/copper–cocatalyzed three-component assembly of readily available aryl iodides, allenes, and aldimine esters by simply tuning the chiral ligands of the palladium and copper catalysts.

中文翻译：

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通过对映体和 Z / E 选择性催化立体发散获得非天然 α-氨基酸


烯烃合成中碳-碳双键的 Z 和 E 构型的精确控制长期以来一直是合成化学中的一个基本挑战，当同时努力实现对映选择性 [( Z , R ), ( Z , S ), （E，R），（E，S）]。此外，对映体纯的非天然α-氨基酸在有机化学和药物化学中备受追捧。在这项研究中，我们报道了一种配体控制的立体发散合成方法，以高产率合成带有三取代烯烃部分的非天然 α-季胺基酸，并具有优异的对映选择性和 Z/E 选择性。这一成功是通过简单地调整钯和铜催化剂的手性配体，将易于获得的芳基碘化物、丙二烯和醛亚胺酯进行钯/铜助催化的三组分组装来实现的。