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1. (WO2000061575) PROCESS FOR THE PRODUCTION OF INDOLE DERIVATIVES AND INTERMEDIATES THEREFOR

Pub. No.:    WO/2000/061575    International Application No.:    PCT/JP2000/002381
Publication Date: Oct 19, 2000 International Filing Date: Apr 12, 2000
IPC: C07D 401/04
Applicants: EISAI CO., LTD.

SASHO, Manabu

KOMATSU, Yuki

MIYAZAWA, Mamoru

MATSUO, Kimihiro

INOUE, Susumu

UENO, Koshi

Inventors: SASHO, Manabu

KOMATSU, Yuki

MIYAZAWA, Mamoru

MATSUO, Kimihiro

INOUE, Susumu

UENO, Koshi

Title: PROCESS FOR THE PRODUCTION OF INDOLE DERIVATIVES AND INTERMEDIATES THEREFOR
Abstract:
A novel industrially excellent process for the production of 1,4-substituted cyclic amine derivatives useful as drugs; and intermediates therefor. Specifically, a process for the production of indole derivatives (I), characterized by reducing a 1,4-substituted-2-nitrophenyl derivative (VII) into a 1,4-substituted-2-aminophenyl derivative (V), reacting the derivative (V) with an N-substituted-4-piperidone derivative (VI) to form a 1,4-substituted-2-piperidylaminophenyl derivative (IV), cyclizing the derivative (IV) into a 2-oxoindoline derivative (III), halogenating the derivative (III) into a 2-haloindole derivative (II), reducing the derivative (II), and, if necessary, subjecting the resulting product to alcoholysis or aminolysis.