Polymorph of regadenoson and process for preparation thereof

US10392417B2 · kind B2 · utility

Assignee

• Apicore US LLC · US

Inventors

• Ravishanker Kovi · Sparta, US
• Jayaraman Kannapan · Sayla, IN
• Ananda Babu Thirunavakarasu · Sayla, IN
• Piyush Fadadu · Vadodara, IN
• Piyush B. Thumar · Sayla, IN

Key dates

• Filing date: Oct 30, 2017
• Grant date: Aug 27, 2019
• Expiry date: Oct 30, 2037

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07B2200/13
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

Processes are provided for the preparation of a stable polymorphic form C of regadenoson, the process involving steps of a) obtaining a solution of regadenoson in benzyl alcohol solvent, b) maintaining the reaction mixture of step a) to about 10° C. to about 90° C., and c) isolating the stable polymorphic form C of regadenoson. Polymorphic form C may be characterized by an x-ray powder diffraction pattern with peaks at about 6.1, 10.2, 10.6, 19.0 and 25.4.±0.2 degrees 2-theta.