Process for the preparation of 3-acyl-indoles

C - Chemistry – Metallurgy – 07 – D

Patent

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C07D 209/12 (2006.01) C07D 209/42 (2006.01) C07D 403/06 (2006.01)

Patent

CA 2322346

The present invention is concerned with the acylation of indoles, specifically the preparation of 3-acylated indoles which may be further treated to provide indoles having an alternative substituent at the 3-position. The 3-acylated indoles have the formula (I): (See formula I) wherein R = C1-C6 alkyl, C1-C6 alkoxy, C3-C7 cycloalkyl, or aryl optionally substituted by one or more of hydroxy, C1-C4 alkyl, C1-C4 alkoxy, fluoro, fluoro (C1-C4) alkyl and fluoro(C1-C4)alkoxy and X is hydrogen or one or more substituents independently selected from cyano, halogen, nitro, C1-C6 alkyl, C1-C6 alkoxy, C3-C7 cycloalkyl and aryl optionally substituted by one or more of cyano, halogen, nitro, C1-C4 alkyl, C1-C4 alkoxy, fluoro (C1-C4) alkyl and fluoro(C1-C4)alkoxy; or wherein R is carboxybenzyl-2- pyrrolidinyl and X is 5-bromo.

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