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Browse Prior Art Database

Vortioxetine HCl polymorphs

IP.com Disclosure Number: IPCOM000248459D
Publication Date: 2016-Dec-01
Document File: 17 page(s) / 1M

Publishing Venue

The IP.com Prior Art Database

Abstract

The present disclosure relates to a crystalline form-M1, M2, M3, M4 and M5 of vortioxetine hydrochloride and also relates to process for the preparation of the same.

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The present disclosure relates to a crystalline form-M1, M2, M3, M4 and M5 of vortioxetine hydrochloride and also relates to process for the preparation of the same. Further relates to process for the preparation of vortioxetine hydrochloride monohydrate.

Vortioxetine hydrobromide, chemically known as 1-[2-(2, 4-Dimethyl-phenylsulfanyl)-phenyl]-piperazine, hydrobromide and structurally represented as formula-I.

In one embodiment, crystalline form-M1 of vortioxetine hydrochloride is characterized by the powder X-ray diffraction having characteristic peak at about 9.4, 18.9 and 28.4 (±) 0.2° 2-theta.

In one more embodiment, crystalline form-M1 of vortioxetine hydrochloride is further characterized by the Powder X-ray diffraction having peaks at about 9.4, 14.5, 16.4, 17.6, 18.9, 20.9, 22.5, 23.3 and 28.4 (±) 0.2° 2-theta.

In one embodiment, crystalline form-M2 of vortioxetine hydrochloride is characterized by the powder X-ray diffraction having characteristic peak at about 12.5, 16.5 and 20.4 (±) 0.2° 2-theta.

In one more embodiment, crystalline form-M2 of vortioxetine hydrochloride is further characterized by the Powder X-ray diffraction having peaks at about 12.5, 16.5, 20.4, 22.1, 23.2 and 26.0 (±) 0.2° 2-theta.

In one embodiment, crystalline form-M3 of vortioxetine hydrochloride is characterized by the powder X-ray diffraction having characteristic peak at about 12.5, 16.5 and 20.4 (±) 0.2° 2-theta.

In one more embodiment, crystalline form-M3 of vortioxetine hydrochloride is further characterized by the Powder X-ray diffraction having peaks at about 10.8, 12.5, 14.0, 16.5, 17.0, 20.4, 22.1, 22.7, 23.2 and 25.0 (±) 0.2° 2-theta.

In one embodiment, crystalline form-M4 of vortioxetine hydrochloride is characterized by the powder X-ray diffraction having characteristic peak at about 12.4, 16.4 and 20.3 (±) 0.2° 2-theta.

In one more embodiment, crystalline form-M4 of vortioxetine hydrochloride is further characterized by the Powder X-ray diffraction having peaks at about 12.4, 16.4, 20.3, 23.1 and 25.9 (±) 0.2° 2-theta.

In one embodiment, crystalline form-M5 of vortioxetine hydrochloride is characterized by the powder X-ray diffraction having characteristic peak at about 12.5, 17.0, 20.4 and 22.7(±) 0.2° 2-theta.

In one more embodiment, crystalline form-M5 of vortioxetine hydrochloride is further characterized by the Powder X-ray diffraction having peaks at about 10.8, 12.5, 16.5, 17.0, 20.4, 22.1, 22.7 and 28.4 (±) 0.2° 2-theta.

Another aspect of the present disclosure is to provide process for the preparation of vortioxetine hydrochloride monohydrate comprising the steps of:

a)      dissolving vortioxetine hydrochloride in a water, water miscible organic solvent or mixture thereof,

b)      optionally heating the reaction mass up to 65°C,

c)      cooling the reaction mass at 0-30°C, and

d)      isolating th...