INDOLE CROSS-COUPLING METHOD Russian patent published in 2011 - IPC C07D209/24 C07D401/04 

Abstract RU 2430916 C2

FIELD: chemistry.

SUBSTANCE: invention relates to a method of producing a compound of general formula 1

by reacting a substituted indole derivative I'

with a heteroarylzinc halide of formula: or a diheteroarylzinc of formula:

where: L denotes Br, Cl; R denotes (C1-C8)alkyl; X denotes (C3-C8)cycloalkyl; Y denotes a 6-member heteroaryl with one or two N atoms; Z denotes HO2C-, (C1-C8)alkyl-O2C-, (C1-C6)alkyl-HNC(O)-, or in the presence of a Pd metal catalyst, a ligand selected from Ph3P, n-Tol3P, Cy3P, tpet-Bu3P, Cy2P(Ph-Ph), dppfh and dppb, in a solvent selected from tetrahydrofuran, dimethylformamide, N-methylpyrrolidone or any other combination thereof, at temperature between ambient temperature and 100°C. The invention also describes intermediate compounds.

EFFECT: high efficiency of the method.

12 cl, 3 dwg, 2 tbl, 4 ex

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RU 2 430 916 C2

Authors

Kkhodabokus Akhmad

Li Gujshehn

Lu Chzhisjuj

Roshangar Frank

Senanajake Kris Kh'Ju

Shehn' Min

Dates

2011-10-10Published

2005-03-07Filed