	US 12,331,053 B2
	Method for obtaining amorphous remimazolam besylate
Carles Sánchez Casals, Barcelona (ES); Alicia Dobarro Rodríguez, Barcelona (ES); and Sergio Carneado Moreno, Barcelona (ES)
Assigned to MOEHS IBERICA, S.L., Barcelona (ES)
Appl. No. 17/627,275
Filed by MOEHS IBERICA, S.L., Barcelona (ES)
PCT Filed Jul. 21, 2020, PCT No. PCT/EP2020/070528 § 371(c)(1), (2) Date Jan. 14, 2022, PCT Pub. No. WO2021/013826, PCT Pub. Date Jan. 28, 2021.
Claims priority of application No. 201930677 (ES), filed on Jul. 22, 2019.
Prior Publication US 2022/0402923 A1, Dec. 22, 2022
Int. Cl. C07D 487/04 (2006.01)

CPC C07D 487/04 (2013.01)

18 Claims

1. A method for preparing amorphous remimazolam besylate comprising the following steps:

a) providing a solution consisting essentially of remimazolam besylate and a solvent selected from the group consisting of water-miscible organic solvent, water, and mixtures thereof, and

b) lyophilizing the solution provided in step a), wherein the lyophilization comprises

b1) freezing the solution provided in step a) at a temperature below −45° C., and

b2) removing the solvent from the product obtained in step b1) by means of heating from the temperature of said product to a temperature of 10° C. to 40° C., at a pressure of less than 101325 Pa and for a time period of less than 5 days.