Unichem Laboratories Limited

Yogesh Subhash Patil

Dhananjay Govind Sathe

Arijit Das

Nilesh L Bonde

Ankush Sampat Kekan

Vishal Kulkarni

Prafulla Nagawade

Tushar Patil

The present invention is related to an improved process for the preparation and purification of crystalline Vortioxetine hydrobromide of Formula-I. The process according to present invention is operationally simple and suitable for industrial application which will avoid hazardous chemicals and eliminate column chromatography to get ICH quality of pharmaceutically acceptable active pharmaceutical ingredient having snow white appearance.

Process for preparation and purification of vortioxetine hydrobromide

The present disclosure is related to an improved and efficient process for preparation of (3R,4R)-(1-benzyl-4-methylpiperidin-3-yl)-methylamine which comprises: (a) N-acylation of 3-Amino-4-methyl pyridine; (b) Quarternization of 3-Acetylamino-4-methyl pyridine using benzyl halide; (c) Partial reduction of quarternized 3-Acetylamino-4-methyl pyridine by Sodium borohydride in Methanol or water; (d) Hydrolysis of partially reduced product to 1-Benzyl-4-methylpiperidin-3-one in presence of acid; (e) Reductive amination of 1-Benzyl-4-methylpiperidin-3-one using Methanolic methylamine in presence of Titanium(IV) isopropoxide in Methanol; (f) Resolution of 1-Benzyl-4-methylpiperidin-3-yl)-methylamine using Ditoluoyl (L) tartaric acid to get (3R,4R)-(1-benzyl-4-methylpiperidin-3-yl)-methylamine. The disclosure is also related to novel intermediates: wherein R, R' and X are as described in the specification.

Process for the preparation of (3R,4R)-(1-benzyl-4-methylpiperidin-3-yl)-methylamine

The present invention is related to an improved and efficient process for preparation of (3R,4R)-(1-benzyl-4-methylpiperidin-3-yl)-methylamine which comprises: wherein R, R' and X are as described in the specification.

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Aurangabad, India

Yogesh Subhash Patil