Diastereoselective Synthesis of beta-Heteroaryl syn-alpha-Methyl-beta-Amino Acid Derivatives via a Double Chiral Auxiliary Approach

[摘要]：The addition of the SuperQuat enolate to five- and six-membered heterocyclic tert-butyl sulfinimines led to a high syn-selectivity of up to 99:1 in good to excellent yields. The reaction Is tentatively proposed to proceed through an open-chain transition state with the presence of an alpha-heteroatom on the sulfinimine leading to high diastereoselectivities. The adducts were derivatized to beta-amino esters and amides in a facile manner.

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