Combinatorial synthesis of libraries of indole derivatives.
The synthesis of two indole derivative libraries is described. 2-Acyl-3-amino-indoles 4 can easily be accessed by treatment of the intermediates 3 with 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 purified by reversed phase column chromatography and obtained in multi-milligram quantities in acceptable yields.
Nettekoven
M
M
F. Hoffmann-La Roche Ltd, Pharmaceutical Research, Discovery Chemistry-Lead Generation, CH-4070, Basel, Switzerland. matthias.nettekoven@roche.com
D002851:Chromatography, High Pressure Liquid; D007211:Indoles / Q000138:chemical synthesis* / Q000737:chemistry; D008968:Molecular Conformation
D007211:Indoles