Journal
ORGANIC & BIOMOLECULAR CHEMISTRY
Volume 13, Issue 2, Pages 520-526Publisher
ROYAL SOC CHEMISTRY
DOI: 10.1039/c4ob01627k
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Funding
- JSPS KAKENHI [23790017, 25460018]
- Platform for Drug Discovery, Informatics, and Structural Life Science from the MEXT
- Hoansha foundation
- Grants-in-Aid for Scientific Research [25460018, 25460157, 23790017] Funding Source: KAKEN
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Highly regioselective (3 + 2) cycloadditions of (trifluoromethanesulfonyloxy)benzynes [(triflyloxy)-benzynes] with 1,3-dipoles followed by cross-coupling reactions provided multisubstituted benzo-fused heterocycles. The triflyloxy group at the 3-position of benzynes, and even that at the remote 4-position, greatly affected the regiocontrol of the cycloaddition. These groups also served to install other substituents at their ipso-positions.
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