The patent badge is an abbreviated version of the USPTO patent document. The patent badge does contain a link to the full patent document.

The patent badge is an abbreviated version of the USPTO patent document. The patent badge covers the following: Patent number, Date patent was issued, Date patent was filed, Title of the patent, Applicant, Inventor, Assignee, Attorney firm, Primary examiner, Assistant examiner, CPCs, and Abstract. The patent badge does contain a link to the full patent document (in Adobe Acrobat format, aka pdf). To download or print any patent click here.

Date of Patent:
Nov. 10, 2020

Filed:

Jan. 11, 2018
Applicant:

Unichem Laboratories Limited, Mumbai, IN;

Inventors:

Dhananjay G. Sathe, Thane, IN;

Arijit Das, Kolkata, IN;

Yogesh Subhash Patil, Aurangabad, IN;

Nilesh L. Bonde, Baroda, IN;

Ankush Sampat Kekan, Pune, IN;

Assignee:
Attorney:
Primary Examiner:
Int. Cl.
CPC ...
C07D 211/02 (2006.01); C07D 213/74 (2006.01); C07D 211/56 (2006.01); C07D 211/72 (2006.01); C07D 213/75 (2006.01); C07D 211/98 (2006.01);
U.S. Cl.
CPC ...
C07D 211/02 (2013.01); C07D 211/56 (2013.01); C07D 211/72 (2013.01); C07D 211/98 (2013.01); C07D 213/74 (2013.01); C07D 213/75 (2013.01);
Abstract

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.


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