Regio- and Diastereoselective Cascade Reactions of Bicyclo[1.1.0]butanes: Access to <i>gem</i>-Difluorinated Carbocyclic Rings
<i>gem</i>-Difluorinated carbocyclic rings are attractive motifs in drug development. Herein, we report the transition-metal free cascade reaction of bicyclo[1.1.0]butanes (BCBs) with <i>gem</i>-difluorocyclopropenes for the synthesis of <i>gem</i>-difluorinated carbocyclic rings with excellent regio- and diastereoselectivity. This method was successfully applied to provide a broad range of <i>gem</i>-difluorinated cyclopentenes and cyclopropanes, which could undergo a variety of difluoromethylene (CF<sub>2</sub>) retaining transformations.
Authors
- Dachang Bai (ORCID: https://orcid.org/0000-0001-7342-2966)
- Hao Wu (ORCID: https://orcid.org/0000-0002-0767-4177)
- Wenjie Xu (ORCID: https://orcid.org/0009-0004-3919-6052)
- Zhiyi Zhang (ORCID: https://orcid.org/0000-0001-9118-4092)
Institutions
- Henan Normal University (CN)
Publication Details
- Journal
- Organic Letters
- Published
- 2025-04-17
- DOI
- https://doi.org/10.1021/acs.orglett.5c01132
- Citations
- 4
- Primary Topic
- Fluorine in Organic Chemistry
- Type
- article
- Field-Weighted Citation Impact
- 3.16
Funders
- National Natural Science Foundation of China
- Natural Science Foundation of Henan Province
- Education Department of Henan Province
- Henan Postdoctoral Science Foundation
- Henan Key Laboratory of Organic Functional Molecules and Drug Innovation