Title:
AN IMPROVED PROCESS FOR PREPARATION OF AGOMELATINE
Document Type and Number:
WIPO Patent Application WO/2014/072998
Kind Code:
A9
Abstract:
The present invention provides an improved process for preparing agomelatine of formula (I). The process comprises reacting 7-methoxy tetralone with cyanoacetic acid in an organic solvent to obtain (7-methoxy-3,4-dihydro- 1 -naphthalenyl)acetonitrile of Formula (B); treating compound of Formula (B) with a catalyst to obtain (7-methoxy- 1 - naphthyl)acetonitrile of Formula (C); reducing compound of formula (C) with hydrogen in presence of Raney nickel in ammoniacal methanol medium and subsequently converting to a salt using hydrochloric acid to obtain 2-(7-methoxy- 1 -naphthyI)ethanamine hydrochloride of formula (D); iv) reacting compound of formula (D) with acetic anhydride or acetic chloride in an organic solvent in presence of a base and a catalyst to obtain agomelatine of Formula (I); and optionally purifying agomelatine of Formula (I). The present invention also provides a process for preparing polymorphic Form-I of agomelatine of formula (I) comprising treating agomelatine of formula (I) in a suitable organic solvent; and isolating polymorphic Form-I of agomelatine of formula (I).
Inventors:
DWIVEDI SHRI PRAKASH DHAR (IN)
PRASAD ASHOK (IN)
SHAH NIRAJ SHYAMLAL (IN)
PATEL MAYUR RAMNIKBHAI (IN)
PRASAD ASHOK (IN)
SHAH NIRAJ SHYAMLAL (IN)
PATEL MAYUR RAMNIKBHAI (IN)
Application Number:
PCT/IN2013/000682
Publication Date:
January 15, 2015
Filing Date:
November 06, 2013
Export Citation:
Assignee:
CADILA HEALTHCARE LTD (IN)
International Classes:
C07C213/02; C07C231/02; C07C253/30
Attorney, Agent or Firm:
SUBRAMANIAM, Hariharan et al. (Central Square Suite-328,,Plaza III, 20 Manoharlal Khurana Mar, Bara Hindu Rao Delhi - 6, IN)
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