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伯胺的连续流合成:用三氯硅烷对脂肪族和芳香族硝基衍生物进行无金属还原。

Continuous-flow synthesis of primary amines: Metal-free reduction of aliphatic and aromatic nitro derivatives with trichlorosilane.

作者信息

Porta Riccardo, Puglisi Alessandra, Colombo Giacomo, Rossi Sergio, Benaglia Maurizio

机构信息

Dipartimento di Chimica, Università di Milano, Via Golgi 19, 20133, Milano, Italy.

出版信息

Beilstein J Org Chem. 2016 Dec 5;12:2614-2619. doi: 10.3762/bjoc.12.257. eCollection 2016.

Abstract

The metal-free reduction of nitro compounds to amines mediated by trichlorosilane was successfully performed for the first time under continuous-flow conditions. Aromatic as well as aliphatic nitro derivatives were converted to the corresponding primary amines in high yields and very short reaction times with no need for purification. The methodology was also extended to the synthesis of two synthetically relevant intermediates (precursors of baclofen and boscalid).

摘要

首次在连续流动条件下成功实现了由三氯硅烷介导的硝基化合物无金属还原为胺的反应。芳香族和脂肪族硝基衍生物在极短的反应时间内以高收率转化为相应的伯胺,无需纯化。该方法还扩展到两种具有合成相关性的中间体(巴氯芬和啶酰菌胺的前体)的合成。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2393/5238609/c5528549aa79/Beilstein_J_Org_Chem-12-2614-g002.jpg

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