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Process for the preparation of amorphous Canagliflozin

IP.com Disclosure Number: IPCOM000241839D
Publication Date: 2015-Jun-03
Document File: 2 page(s) / 185K

Publishing Venue

The IP.com Prior Art Database

Abstract

Process for the preparation of amorphous canagliflozin by distillation, lyophilisation, spray drying and anti-solvent methods.

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"Process for the preparation of amorphous Canagliflozin"

Canagliflozin is chemically known as (2S, 3R 4R, 5S,6R)-2-{3-[5-[4-Fluoro-phenyl)-thiophen-2- ylmethyl]-4-methyl-phenyl}-6-hydroxymethyl-tetrahydro-pyran-3,4,5-triol and structurally represented as:

Canagliflozin is an API that is an inhibitor of SGLT2 and is being developed for the treatment of type 2 diabetes mellitus.

This disclosure is about process for the preparation of amorphous form of Canagliflozin Comprising the steps of dissolving Canagliflozin in a solvent, removing the solvent, and Isolating amorphous Canagliflozin.

In another process for the preparation of amorphous form of Canagliflozin comprising the steps of dissolving Canagliflozin in a solvent, adding anti-solvent, and Isolating amorphous Canagliflozin.

Fig.1 represents the amorphous form of Canagliflozin.

Example 1 (ATFD)

Dissolved Canagliflozin (100 g) in methylene dichloride (1000 ml) and stirred for clean solution. Fed the mass into ATFD with dosing pump flow rate of 15 rpm at a temperature of 45-60° C and vacuum of 650±50 mm in Hg. Slowly collected the material from the receiver. Unload the material and dried at 45° C under vacuum (650±50 mm in Hg) t o give 90 g of amorphous Canagliflozin.

Example 2 (Spray Drying)

Dissolved Canagliflozin (100 g) in methylene dichloride (1000 ml) and stirred for clean solution. Fed the mass into spray dryer at 45-60° C and vacuu m 650±50 mm in Hg. Slowly collected the material from receiver. Un...