1-阿扎比环丁烷的菌株释放功能化合成对映控制氮杂苷文库

IF 15.6 1区化学 Q1 CHEMISTRY, MULTIDISCIPLINARY

Journal of the American Chemical Society Pub Date : 2025-06-11 DOI:10.1021/jacs.5c07227

Michael Bielecki, Molhm Nassir, Hayden A. Sharma, Nathanyal J. Truax, Nicholas Raheja, Ty M. Thompson, Tamara El-Hayek Ewing, Bruno Melillo, Benjamin F. Cravatt* and Phil S. Baran*,

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引用次数: 0

摘要

本发明公开了一种简单、模块化和可编程的方法，通过菌株释放功能化来获得复杂的立体氮杂丁。所开发的合成方法使平行合成立体氮杂丁成为可能，否则将难以生产。考虑到这些结构的特殊性质，一组用于基于活性的蛋白质分析的立体探针被制备和评估，揭示了人类癌细胞中的蛋白质，这些蛋白质配体具有明确的立体和化学选择性。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

Enantiocontrolled Azetidine Library Synthesis via Strain-Release Functionalization of 1-Azabicyclobutanes

查看原文本刊更多论文

Enantiocontrolled Azetidine Library Synthesis via Strain-Release Functionalization of 1-Azabicyclobutanes

A simple, modular, and programmable approach to access complex stereopure azetidines through strain-release functionalization is disclosed. The synthetic methods developed enable the parallel synthesis of stereodefined azetidines that would be otherwise laborious to produce. Given the privileged nature of these structures, a set of stereoprobes for use in activity-based protein profiling was prepared and evaluated, revealing proteins in human cancer cells, which were liganded with clear stereo- and chemo-selectivity.

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来源期刊

Journal of the American Chemical Society 化学-化学综合

CiteScore

24.40

自引率

6.00%

发文量

2398

审稿时长

1.6 months

期刊介绍： The flagship journal of the American Chemical Society, known as the Journal of the American Chemical Society (JACS), has been a prestigious publication since its establishment in 1879. It holds a preeminent position in the field of chemistry and related interdisciplinary sciences. JACS is committed to disseminating cutting-edge research papers, covering a wide range of topics, and encompasses approximately 19,000 pages of Articles, Communications, and Perspectives annually. With a weekly publication frequency, JACS plays a vital role in advancing the field of chemistry by providing essential research.