ES266424A1 - Procedure for the preparation of new indolor derivatives (Machine-translation by Google Translate, not legally binding) - Google Patents

Abstract

Process for the preparation of new indole derivatives of the formula I ** (See formula) ** in which R1 = H, halogen, OH, alkyl or alkoxy, R2 = alkyl, R3, R4 and R5 are the same or different and mean an aryl radical (which is optionally substituted by halogen), or an alkyl or alkenyl radical (in which case two of these radicals can be linked together, optionally by means of a carbon atom. N), a cycloalkyl radical or a heterocyclic radical (in which case one of the radicals R3 to R5 can also mean H, Cl, Br or OH), Y = -O-CO-, -O-, -O-CH2- or -NH-CO-, characterized by the fact that a) an indole derivative of the formula is reacted ** (See formula) ** in which R1 and R2 have the meaning indicated above, X = OH, O-alkali metal, halogen, O-acyl, NH2 or a sulphonic radical, with a substituted acetic acid of formula III ** (See formula) ** wherein R3, R4 and R5 have the meaning indicated above, with one of their reactable derivatives or with a halogen compound of the formula IV ** (See formula) ** wherein R3, R4 and R5 have the meaning indicated above, and Z = halogen or halogen-CH2- or b) a compound of the formula I containing double bonds in position 2,3 and/or in the benzene nucleus is converted, by hydrogenation, into the corresponding saturated compound, or c) is introduced into a compound of the formula I that does not contain one or more of the radicals R1 to R5, the missing substituent (s), or other substituents are transformed into the radicals R1 to R5, and optionally d) is transformed a compound of the formula I in its acid addition salt, a quaternary compound or a respective amino-oxide. (Machine-translation by Google Translate, not legally binding)