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Approach to 3-(Cyclo)alkylpiperidines through 'sp3-sp3 via sp2-sp3' Coupling.
- Source :
- Synlett; 2015, Vol. 26 Issue 3, p408-411, 4p
- Publication Year :
- 2015
-
Abstract
- The idea of introducing (cyclo)alkyl substituents at the C-3 atom of the piperidine ring, that is, formal sp<superscript>3</superscript>-sp<superscript>3</superscript> retrosynthetic disconnection, is implemented through a two-step reaction sequence including directed ortho metalation of a pyridine derivative and the subsequent quenching with a carbonyl compound, followed by catalytic hydrogenation. This robust but very efficient method allows for multigram preparation of sp<superscript>3</superscript>-rich 3-(cyclo)alkylpiperidines, which are valuable building blocks for medicinal chemistry and other areas. [ABSTRACT FROM AUTHOR]
Details
- Language :
- English
- ISSN :
- 09365214
- Volume :
- 26
- Issue :
- 3
- Database :
- Complementary Index
- Journal :
- Synlett
- Publication Type :
- Academic Journal
- Accession number :
- 100791889
- Full Text :
- https://doi.org/10.1055/s-0034-1379502