A metal-free protocol for the preparation of amines using ammonia borane under mild conditions,Organic Chemistry Frontiers

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A metal-free protocol for the preparation of amines using ammonia borane under mild conditions
Organic Chemistry Frontiers ( IF 4.6 ) Pub Date : 2022-12-29 , DOI: 10.1039/d2qo01938h
Xinmin Li _{1,

2} , Yue Hu ₂ , Asma M. Alenad ₃ , Bei Zhou ₂ , Zhuang Ma ₂ , Jie Gao ₂ , Rajenahally V. Jagadeesh ₂ , Matthias Beller ₂

Affiliation

A mild and convenient reductive amination protocol for the synthesis of structurally diverse secondary and tertiary amines as well as N-methylated products under metal-free conditions is presented. This one-pot protocol works efficiently at room temperature using ammonia borane as the reductant and is applicable to a wide range of substrates, including chiral amines and amino acid derivatives. The synthetic utility and practicability of this methodology is demonstrated by gram-scale reactions and selected synthesis of current drug molecules.

中文翻译：

在温和条件下使用氨硼烷制备胺的无金属方案

提出了一种温和方便的还原胺化方案，用于在无金属条件下合成结构多样的仲胺和叔胺以及N-甲基化产物。这种一锅法在室温下有效地使用氨硼烷作为还原剂，适用于多种底物，包括手性胺和氨基酸衍生物。该方法的合成实用性和实用性通过克级反应和当前药物分子的选择合成得到证明。

更新日期：2022-12-29

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