Base Mediated 7-exo-dig Intramolecular Cyclization of Betti-propargyl Precursors: An Efficient Approach to 1,4-oxazepine Derivatives.

IF 1.7 4区化学 Q3 CHEMISTRY, ORGANIC

Current organic synthesis Pub Date : 2025-02-11 DOI:10.2174/0115701794353226241209175136

Rozita Yazzaf, Mina Asadi, Mohammad Mahdavi

引用次数: 0

Abstract

Introduction: 1,4-oxazepine is a significant structural motif found in several bio-active molecules used in the treatment of diseases such as psychotic disorders.

Methods: Therefore, developing novel methodologies for its preparation is of great interest to medicinal chemists.

Results: These seven-membered heterocycles are generated through the intramolecular cy-clization of Betti bases, which are propargylated using propargyl bromide as the source of the triple bond in the presence of a base.

Conclusion: This efficient and straightforward protocol proceeds under mild, metal-free conditions and has been shown to be applicable to a broad range of aldehydes and 2-aminopyridines.

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碱介导的β -丙炔前体分子内7-外环化：1,4-恶氮平衍生物的一种有效方法。

1,4-恶氮平是一种重要的结构基序，存在于一些生物活性分子中，用于治疗精神疾病等疾病。方法：因此，开发新的制备方法是药物化学家非常感兴趣的。结果：这些七元杂环是通过Betti碱的分子内环化生成的，在碱存在的情况下，以丙炔溴为三键源进行丙炔基化。结论：该方法在温和、无金属的条件下进行，并已被证明适用于广泛的醛类和2-氨基吡啶。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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来源期刊

Current organic synthesis 化学-有机化学

CiteScore

3.40

自引率

5.60%

发文量

审稿时长

6-12 weeks

期刊介绍： Current Organic Synthesis publishes in-depth reviews, original research articles and letter/short communications on all areas of synthetic organic chemistry i.e. asymmetric synthesis, organometallic chemistry, novel synthetic approaches to complex organic molecules, carbohydrates, polymers, protein chemistry, DNA chemistry, supramolecular chemistry, molecular recognition and new synthetic methods in organic chemistry. The frontier reviews provide the current state of knowledge in these fields and are written by experts who are internationally known for their eminent research contributions. The journal is essential reading to all synthetic organic chemists. Current Organic Synthesis should prove to be of great interest to synthetic chemists in academia and industry who wish to keep abreast with recent developments in key fields of organic synthesis.