The in situ oxidation-Wittig reaction of alpha-hydroxyketones.

In situ oxidation-Wittig methodology has been applied to alpha-hydroxyketones avoiding the problems normally associated with alpha-ketoaldehydes; the procedure is practically simple, and in many cases gives high yields of the product gamma-ketocrotonates; the procedure has also been successfully utilised with ethyl glycolate and glycolaldehyde dimer.

8-Methoxyquinoline-5-carboxamides as PDE4 inhibitors: a potential treatment for asthma.

A series of bicyclic heteroaryl ring systems was considered as a replacement for the 3-cyclopentyloxy-4-methoxyphenyl moiety in rolipram resulting in the discovery of 8-methoxyquinoline-5-carboxamides as potent inhibitors of phosphodiesterase type 4 (PDE4).

Synthesis and profile of SCH351591, a novel PDE4 inhibitor.

The syntheses and pharmacological profiles of some 2-trifluoromethyl-8-methoxyquinoline-5-carboxamides are described. SCH351591 is a potent selective inhibitor of phosphodiesterase type 4 (PDE4).