Enantioselective β-C(sp3)–H Nucleophilic Tosylation of Native Amides: A Synthetic Platform for Chiral Methyl Stereocenters DOI
Yuxin Ouyang, D. Quang Phan, Nikita Chekshin

и другие.

Journal of the American Chemical Society, Год журнала: 2025, Номер unknown

Опубликована: Май 31, 2025

Enantioselective oxygenation of unactivated C(sp3)-H bonds via asymmetric metalation remains an unsolved challenge. Herein we report the development a Pd-catalyzed, enantioselective tosylation native amides with NaOTs as nucleophile, representing rare example C-H functionalization nucleophilic coupling partner. High enantioselectivity in this reaction is achieved by chiral monoprotected amino sulfonamide (MPASA) ligands. Substantial enhancement silver salt additives was also observed. Through desymmetrization readily available isopropyl moiety, structurally diverse β-tosylated bearing α-methyl stereocenter were obtained high yield and enantioselectivity, which complements current enzymatic method for making Roche ester synthon. The tosylated products are highly versatile building blocks further diversifications nitrogen, oxygen, other nucleophiles, thus providing platform constructing methyl stereocenters.

Язык: Английский

Photocatalytic Pyridyl-carbamoylation of Alkenes for Accessing β-Pyridyl Amides DOI
Jian Cui, Zhikai Li, Yun Mao

и другие.

Organic Letters, Год журнала: 2025, Номер unknown

Опубликована: Март 7, 2025

The β-pyridyl amide is a critical scaffold in medical discovery yet lacks efficient synthetic methods. Here, we describe, for the first time, visible-light-induced, redox-neutral radical cross-coupling reaction involving alkenes, oxamic acids, and cyanopyridines that offers versatile assembly of β-pyridylamides. This approach features mild conditions, high step efficiency, substrate breadth, providing green strategy alkene pyridyl-carbamoylation. Achieving this transformation relies on catalytic system, which adeptly avoids competing nucleophilic carbamoyl with electrophilic pyridyl radical, enabling three-component tandem process chemoselectivity.

Язык: Английский

Процитировано

0

Nickel-Catalyzed C(sp3)–C(sp3) Cross-Coupling of Carboxamides and Unactivated Alkyl Iodides DOI

Haochen Li,

Guohua Ren, Xi Chen

и другие.

The Journal of Organic Chemistry, Год журнала: 2025, Номер unknown

Опубликована: Май 22, 2025

The construction of C(sp3)-C(sp3) bonds through cross-coupling reactions unactivated alkyl halides and C-radical precursors presents a significant challenge in organic synthesis. Herein, we report strategy for the formation using as alkylation reagents via 1,5-hydrogen atom transfer (HAT) process. proceed under mild conditions, demonstrating remarkable tolerance diverse array functional groups. This method possesses potential to expand new pathways

Язык: Английский

Процитировано

0

Enantioselective β-C(sp3)–H Nucleophilic Tosylation of Native Amides: A Synthetic Platform for Chiral Methyl Stereocenters DOI
Yuxin Ouyang, D. Quang Phan, Nikita Chekshin

и другие.

Journal of the American Chemical Society, Год журнала: 2025, Номер unknown

Опубликована: Май 31, 2025

Enantioselective oxygenation of unactivated C(sp3)-H bonds via asymmetric metalation remains an unsolved challenge. Herein we report the development a Pd-catalyzed, enantioselective tosylation native amides with NaOTs as nucleophile, representing rare example C-H functionalization nucleophilic coupling partner. High enantioselectivity in this reaction is achieved by chiral monoprotected amino sulfonamide (MPASA) ligands. Substantial enhancement silver salt additives was also observed. Through desymmetrization readily available isopropyl moiety, structurally diverse β-tosylated bearing α-methyl stereocenter were obtained high yield and enantioselectivity, which complements current enzymatic method for making Roche ester synthon. The tosylated products are highly versatile building blocks further diversifications nitrogen, oxygen, other nucleophiles, thus providing platform constructing methyl stereocenters.

Язык: Английский

Процитировано

0