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苯乙烯的光催化分子间溴硝基烷基化反应:环丙胺衍生物的合成及其作为 LSD1 抑制剂的评价

Photocatalytic intermolecular bromonitroalkylation of styrenes: synthesis of cyclopropylamine derivatives and their evaluation as LSD1 inhibitors.

作者信息

Kim Darong, Jeon Hui-Jeon, Kwak Yoonna, Lee Sun Joo, Nam Tae-Gyu, Yu Ji Hoon, An Hongchan, Hong Ki Bum

机构信息

New Drug Development Center (NDDC), Daegu-Gyeongbuk Medical Innovation Foundation (DGMIF) 80 Cheombok-ro, Dong-gu Daegu 41061 Republic of Korea

Department of Pharmacy, Institute of Pharmaceutical Science and Technology, Hanyang University ERICA Ansan Gyeonggi-do 15588 Republic of Korea.

出版信息

RSC Adv. 2024 Jan 2;14(2):831-835. doi: 10.1039/d3ra07830b.

Abstract

A mild and efficient method for photoredox-catalyzed bromonitroalkylation of alkenes is described herein. In this reaction, bromonitromethane serves as a source of both nitroalkyl and bromine for direct and regioselective formation of C-Br and C-C bonds from alkenes, and additional cyclization provides C-C bonds to the cyclopropylamine core as an LSD1 inhibitor.

摘要

本文描述了一种温和且高效的光氧化还原催化烯烃溴代硝基烷基化方法。在该反应中,溴硝基甲烷作为硝基烷基和溴的来源,用于从烯烃直接且区域选择性地形成C-Br键和C-C键,并且额外的环化反应为作为LSD1抑制剂的环丙胺核心提供C-C键。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/27af/10759170/583a3405203b/d3ra07830b-s1.jpg

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