4,4-Difluorospiro[2.2]pentan-1-yl – A Fluorinated Substituent To Expand the Synthetic and Medicinal Chemists’ Toolbox,European Journal of Organic Chemistry

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4,4-Difluorospiro[2.2]pentan-1-yl – A Fluorinated Substituent To Expand the Synthetic and Medicinal Chemists’ Toolbox
European Journal of Organic Chemistry ( IF 2.5 ) Pub Date : 2022-08-04 , DOI: 10.1002/ejoc.202200863
Kostiantyn P. Melnykov ₁ , Olena V. Voloshyna ₁ , Bohdan V. Vashchenko ₁ , Oleksandr P. Demchuk ₂ , Oleksandr V. Hryshchuk ₂ , Oleksandr O Grygorenko ₁

Affiliation

Scalable and diastereoselective synthetic approach to 4,4-difluorospiro[2.2]pentan-1-yl derivatives by the difluorocyclopropanation of (2-methylenecyclopropyl)methanol and further chemical modifications were disclosed. Structural features, pK_a, logP, and aqueous solubility of the products were established and compared with those of non-fluorinated and 2,2-difluorinated analogs, as well as monocyclic gem-difluorinated counterparts.

中文翻译：

4,4-Difluorospiro[2.2]pentan-1-yl – 一种氟化取代基，可扩展合成和药物化学家的工具箱

公开了通过 (2-亚甲基环丙基) 甲醇的二氟环丙烷化和进一步的化学修饰制备 4,4-二氟螺[2.2]戊-1-基衍生物的可扩展和非对映选择性合成方法。建立了产品的结构特征、p K _a、log P和水溶性，并与非氟化和 2,2-二氟化类似物以及单环偕二氟化对应物进行了比较。

更新日期：2022-08-04

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