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Synthesis of 1,3-disubstituted bicyclo[1.1.0]butanes via directed bridgehead functionalization

Abstract:
Bicyclo[1.1.0]butanes (BCBs) are increasingly valued as intermediates in ‘strain release’ chemistry for the synthesis of substituted four membered rings and bicyclo[1.1.1]pentanes, with applications including bioconjugation processes. Variation of the BCB bridgehead substituents can be challenging due to the inherent strain of the bicyclic scaffold, often necessitating linear syntheses of specific BCB targets. Here we report the first palladium catalyzed cross-coupling on pre-formed BCBs which enables a ‘late stage’ diversification of the bridgehead position, and the conversion of the resultant products into a range of useful small ring building blocks.
Publication status:
Published
Peer review status:
Peer reviewed

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Publisher copy:
10.1039/d1sc01836a

Authors


Publisher:
Royal Society of Chemistry
Journal:
Chemical Science More from this journal
Volume:
12
Issue:
21
Pages:
7480-7485
Publication date:
2021-04-27
Acceptance date:
2021-04-26
DOI:
EISSN:
2041-6539
ISSN:
2041-6520


Language:
English
Keywords:
Pubs id:
1177181
Local pid:
pubs:1177181
Deposit date:
2021-06-22
ARK identifier:

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