Work

Generation and Use of Bicyclo[1.1.0]butyllithium under Continuous Flow Conditions

Year: 2025

Type: article

Abstract: The bicyclo[1.1.0]butyl scaffold has emerged as a valuable bioisostere in drug discovery programs. Here, we present a streamlined approach for the generation of bicyclo[1.1.0]butyllithium and its functionalization with various classes of electrophiles in a one-flow process, eliminating the need for intermediate isolation. In comparison to traditional batch processes, the flow method allows the use of a single organolithium reagent instead of two and operates at significantly higher temperatures (0 °C versus -78 °C), enhancing both practicality and scalability.

Source: Organic Letters

DOI: 10.1021/acs.orglett.5c00705

Authors: Elena Graziano, Marco Colella, Marcus Baumann, Renzo Luisi

Institutions: University College Dublin, University of Bari Aldo Moro

Language: English

Topic: Coordination Chemistry and Organometallics

Subfield: Organic Chemistry

Field: Chemistry

Domain: Physical Sciences

Open Access status: hybrid

Estimated APC paid: $4,500

Funders: HORIZON EUROPE Framework Programme, Research Ireland