Azetidines are increasingly important heterocycles found in a variety of natural products and pharmaceutical compounds. Protected 3-haloazetidines, widely used and versatile building blocks in medicinal chemistry, have been prepared in a one-pot, gram-scale strain-release reaction of 1-azabicyclo[1.1.0]butane from commercially available starting materials. These intermediates were subsequently used to prepare a series of high value azetidine-3-carboxylic acid derivatives including the first reported synthesis of 1-(tert-butoxycarbonyl)-3-((trifluoromethyl)thio)azetidine-3-carboxylic acid.

中文翻译：

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受保护的 3-卤代氮杂环丁烷的改进的克级合成：氮杂环丁烷-3-羧酸的快速多样化合成

氮杂环丁烷是在各种天然产物和药物化合物中发现的越来越重要的杂环。受保护的 3-卤代氮杂环丁烷是药物化学中广泛使用的通用构件，已在 1-氮杂双环 [1.1.0] 丁烷的一锅、克级应变释放反应中从市售原料制备。这些中间体随后用于制备一系列高价值的氮杂环丁烷-3-羧酸衍生物，包括首次报道的 1-(叔丁氧基羰基)-3-((三氟甲基)硫代)氮杂环丁烷-3-羧酸的合成。