Novel synthetic routes suitable for constructing benzopyrone combinatoriallibraries

A series of O-(t-butylsilyloxy)benzoyl chlorides generated from the corresp onding silyl esters were coupled with a range of terminal alkynes to afford the corresponding alkynyl ketones. The alkynyl ketones were converted to e naminoketones and then cyclized to yield the desired benzopyrone ring syste m. This synthetic protocol utilizes readily available starting materials, m ild and high yielding reactions with good functional group tolerance, and i s ideal for developing combinatorial libraries centered around the benzopyr one ring system. (C) 1999 Elsevier Science Ltd. All rights reserved.