Formal Umpolung Strategy for the Synthesis of α-Branched Amides via α-Sulfenylnitro Compounds.

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Tác giả: Mao Shintani, Shinya Shiomi, Masahiro Yoshida

Ngôn ngữ: eng

Ký hiệu phân loại: 583.95 *Scrophulariales

Thông tin xuất bản: Germany : Chemistry (Weinheim an der Bergstrasse, Germany) , 2025

Mô tả vật lý:

Bộ sưu tập: NCBI

ID: 472893

Amide compounds are essential structural motifs found in natural products, pharmaceuticals, peptides and materials. A novel formal umpolung strategy for an efficient synthesis of α-branched amides was developed, employing nitroalkenes, Grignard reagents and amines as reacting components. The synthesis involves the formation of α-sulfenylnitro intermediates, which undergo oxidative amidation under optimized conditions using tert-butyl hydroperoxide (TBHP) as an oxidant and K2CO3 as a base. The key intermediate, an α-sulfenylnitro compound, was successfully synthesized in a one-pot operation. This methodology demonstrates a broad substrate scope, accommodating various amines, including primary and secondary amines as well as amino acid derivatives, and yielding the corresponding α-branched amides in high efficiency. The sulfenyl nitro scaffold proved particularly effective, offering both stability and reactivity. The developed process simplifies the preparation of α-branched amides and expands the accessible structural diversity.
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