Synthesis and Use of Bicyclo[1.1.1]pentylaldehyde Building Blocks

Lasányi, Dániel and Máth, Dániel and Tolnai, Gergely L. (2022) Synthesis and Use of Bicyclo[1.1.1]pentylaldehyde Building Blocks. The Journal of Organic Chemistry. ISSN 0022-3263

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Abstract

The bicyclo[1.1.1]pentane (BCP) motif is an emerging scaffold in medicinal chemistry because of its bioisosterism to 1,4- phenylene and 1,2-alkynyl functions. The current drawback of its use is the lack of stable versatile synthetic building blocks. Aldehydes are among the most useful functionalities in organic chemistry. In this paper, a simple one-pot procedure from aryl-halides and [1.1.1]- propellane is described. Preparation of various BCP molecules is conducted to showcase the versatility of these stable intermediates.

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