Catalytic, Enantioselective Aldol Additions to Ketones

Abstract
Catalytic, enantioselective additions of a trichlorosilyl ketene acetal to ketones have been demonstrated. The trichlorosilyl enolate of methyl acetate undergoes a rapid and high-yielding aldol addition to a wide range of ketones (aromatic, olefinic, acetylenic, aliphatic) in the presence of a catalytic amount of pyridine N-oxide. Moreover, in the presence of a catalytic amount (10 mol %) of a chiral bispyridine bis N-oxide (possessing both axial and central chiral elements) the aldol addition takes place again in excellent yield and with good stereoselectivity. The enantioselectivities of the additions are highly variable (7−86% ee) and are strongly dependent on the structure of the ketone acceptor. Aromatic methyl ketones gave the highest selectivity, whereas olefinic ketones were the least selective.

This publication has 17 references indexed in Scilit: