Taming 3-Oxetanyllithium Using Continuous Flow Technology

doi:10.1021/acs.orglett.4c00644

2024-03-28

DOI：10.1021/acs.orglett.4c00644

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摘要

En 中文

The oxetane ring has evolved as a useful bioisostere for dimethyl and carbonyl groups for the improvement of physiochemical properties of drug candidates. Herein, we report the generation and utilization of highly unstable 3-oxetanyllithium as a hitherto unexplored nucleophile leveraging flash technology. A range of different electrophiles are suitable reaction partners in this protocol, and we demonstrate the utility of this protocol in late-stage pharmaceutical analogue synthesis.

Keyword:

DRUG DISCOVERY

OXETANES

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期刊

Organic Letters

IF:

论文数:

3.9W

被引数:

10.0W

机构

universita degli studi di bari aldo moro

学者数:

2.1W

论文数: 1.6W

被引数: 9

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