Asymmetric Aza-Michael/Michael/Mannich Domino Reaction of 2-Aminochalcones and 5-Alkenyl-Thiazolones: Access to Enantioenriched 1,4-Sulfur-Bridged Piperidinone Skeletons.

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Tác giả: Zahid Ahmad Khan, Shweta Rohilla, Vinod K Singh

Ngôn ngữ: eng

Ký hiệu phân loại: 641.584 Gas

Thông tin xuất bản: United States : Organic letters , 2025

Mô tả vật lý:

Bộ sưu tập: NCBI

ID: 112717

 Herein, we disclose a novel organocatalytic approach for the enantioselective synthesis of 1,4-sulfur-bridged piperidinone skeletons via sequential aza-Michael/Michael/Mannich domino reaction of 2-aminochalcones and 5-alkenyl-thiazolones. The one-pot approach catalyzed by a bifunctional squaramide catalyst furnishes bridged polycyclic compounds with five contiguous stereocenters (three tertiary, two heteroquaternary) in excellent yields (up to 95%) and stereochemical outcomes (up to 99% ee and up to >
 20:1 dr). The methodology offers outstanding control on regio- and chemoselectivity, showcasing broad substrate compatibility. Additionally, the reaction is scalable and postsynthetic transformation to a spirothiazolone-tetrahydroquinoline derivative further amplifies the synthetic utility of the methodology.
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