Regioselective Synthesis of Unsymmetric Tetra- and Pentasubstituted Pyrenes with a Strategy for Primary C-Alkylation at the 2-Position

J Org Chem. 2018 Sep 7;83(17):10660-10667. doi: 10.1021/acs.joc.8b01491. Epub 2018 Jul 2.

Abstract

The synthesis of 1,2,4,5- and 1,2,9,10-tetrasubstituted and 1,2,4,5,8-pentasubsutituted pyrenes has been achieved by initially functionalizing the K-region of pyrene. Bromination, acylation, and formylation reactions afford high to moderate levels of regioselectivity, which facilitate the controlled introduction of other functional groups about 4,5-dimethoxypyrene. Access to 4,5-dimethoxypyren-1-ol and 9,10-dimethoxypyren-1-ol enabled a rare, C-2 primary alkyl substitution of pyrene.

Publication types

  • Research Support, U.S. Gov't, Non-P.H.S.