Combinatorial synthesis of libraries of indole derivatives

The synthesis of two indole derivative libraries is described. 2-Acyl-3-ami no-indoles 4 can easily be accessed by treatment of the intermediates 3 wit h bases in a one-pot reaction sequence whereas the reaction of the isolated intermediates 5 (R-3 =aromatic-, heteroaromatic, or cycloalkyl) with acid chlorides yielded the novel indole derivatives 6. The products were purifie d by reversed phase column chromatography and obtained in multi-milligram q uantities in acceptable yields. (C) 2001 Elsevier Science Ltd. All rights r eserved.