Molybdenum-Promoted Synthesis of Isoquinuclidines with Bridgehead CF3 Groups

J Am Chem Soc. 2019 Nov 27;141(47):18890-18899. doi: 10.1021/jacs.9b10781. Epub 2019 Nov 14.

Abstract

The preparation of the complex MoTp(NO)(DMAP)(4,5-η2-(2-trifluoromethyl)pyridine) (DMAP = 4-(dimethylamino)pyridine; Tp = tris(pyrazolyl)borate) is described. The CF3 substituent is found to preclude κ-N coordination, allowing for direct coordination without protection of the nitrogen. The dihapto-coordinate complex can be isolated as a single diastereomer, methylated, and reacted with a range of nucleophiles. Oxidative decomplexation affords the free dihydropyridines in good yield (75-90%). As a demonstration of synthetic utility, a series of novel bridgehead CF3-substituted isoquinuclidines was prepared from these decomplexed dihydropyridines.

Publication types

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