Crystalline form of Eltrombopag free acid

Patent metadata

Field	Value
Publication number	US-10336706-B2
Application number	US-201515508540-A
Country	US
Kind code	B2
Filing date	Sep 2, 2015
Priority date	Sep 5, 2014
Publication date	Jul 2, 2019
Grant date	Jul 2, 2019

Abstract

The present invention relates to crystalline form of Eltrombopag free acid and its process for preparation.

First claim

We claim:

1. A process for the preparation of crystalline Eltrombopag Form H1 having 2θ angle positions at about 6.3, 7.0, 9.0, 11.5, 12.7, 14.2, 20.5, 23.1, 25.5 and 28.6±0.2 degrees, which comprises:
a) dissolving Eltrombopag in dimethyl formamide;
b) heating the solution to reflux at 50-100° C.;
c) cooling the solution to below 35° C. and adding an alcoholic solvent selected from methanol, ethanol, n-butanol, and isopropanol;
d) heating the solution to reflux at 50-100° C. and e) isolating the crystalline Eltrombopag Form H1.

2. A process for the preparation of crystalline Form 1 of Eltrombopag Olamine, which comprises:
a) preparing crystalline Eltrombopag Form H1 according to the method of claim 1 and dissolving said crystalline Eltrombopag Form H1 in tetrahydrofuran;
b) optionally treating with Carbon;
c) adding an alcoholic solution of 2-amino alcohol and ethanol;
d) removing the solvents; and
e) isolating crystalline Eltrombopag Olamine salt Form I.

Assignees

• Hetero Research Foundation

Inventors

• Parthasaradhi Reddy Bandi
• Rathnakar Reddy Kura
• Sambi Reddy Jonnala
• Vamsi Krishna Bandi

Classifications

• C07D231/08

  with oxygen or sulfur atoms directly attached to ring carbon atoms · CPC title

• C07D231/46 Primary

  Oxygen atom in position 3 or 5 and nitrogen atom in position 4 · CPC title

• C07C201/12

  by reactions not involving the formation of nitro groups · CPC title