Expedient Synthesis of 6-Functionalized Azabicyclo[4.1.0]heptane Derivatives,ChemistrySelect

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Expedient Synthesis of 6-Functionalized Azabicyclo[4.1.0]heptane Derivatives
ChemistrySelect ( IF 1.9 ) Pub Date : 2023-12-21 , DOI: 10.1002/slct.202304331
Taras V. Omelian _{1,

2} , Eugeniy N. Ostapchuk _{1,

2} , Alexey V. Dobrydnev _{1,

2} , Oleksandr O. Grygorenko _{1,

2}

Affiliation

A convenient methodology for the preparation of 6-functionalized azabicyclo[4.1.0]heptane-derived building blocks is developed. The common synthetic precursor – tert-butyl 6-(hydroxymethyl)-3-azabicyclo[4.1.0]heptane-3-carboxylate was obtained in 4 steps starting from readily available 4-hydroxymethyl pyridine. Other 6-functionalized and 3,6-difunctionalized azabicyclo[4.1.0]heptane-derived building blocks (including novel bicyclic γ-amino acid) were prepared in short synthetic pathways through 1–3 steps.

中文翻译：

6-官能化氮杂双环[4.1.0]庚烷衍生物的便捷合成

开发了一种制备 6-官能化氮杂双环[4.1.0]庚烷衍生结构单元的便捷方法。常见的合成前体 - 6-（羟甲基）-3-氮杂双环[4.1.0]庚烷-3-甲酸叔丁酯是从容易获得的 4-羟甲基吡啶开始，分 4 个步骤获得的。其他 6-官能化和 3,6-双官能化氮杂双环[4.1.0]庚烷衍生结构单元（包括新型双环 γ-氨基酸）通过 1-3 个步骤以短合成途径制备。

更新日期：2023-12-22

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