公开(公告)号：US20220402923A1

公开(公告)日：2022-12-22

申请号：US17627275

申请日：2020-07-21

Applicant: MOEHS IBERICA S.L.

Inventor： Carles SÁNCHEZ CASALS ,  Alicia DOBARRO RODRÍGUEZ ,  Sergio CARNEADO MORENO

IPC: C07D487/04

Abstract: The present invention relates to a lyophilization method for obtaining amorphous remimazolam besylate without contamination of crystalline material of said product.

公开(公告)号：US20230092143A1

公开(公告)日：2023-03-23

申请号：US17814815

申请日：2022-07-25

Applicant: MOEHS IBERICA, S.L.

Inventor： Abdeslam AKHATOU ,  Alicia DOBARRO RODRÍGUEZ

IPC: C07D401/12 ,  C07C201/14 ,  C07D239/34 ,  C07D239/36

Abstract: A method is for the synthesis of 2,4-dimethylpyrimidin-5-ol, which can be used as an intermediate compound in the synthesis of Lemborexant. The method includes reacting a nitrophenyl compound with N,N-dimethylformamide diethyl acetal.

公开(公告)号：US20220411382A1

公开(公告)日：2022-12-29

申请号：US17755412

申请日：2020-03-10

Applicant: MOEHS IBERICA, S.L.

Inventor： Roberto BALLETTE ,  Oscar JIMÉNEZ ALONSO ,  Elena GARCÍA GARCÍA ,  Alicia DOBARRO RODRÍGUEZ

IPC: C07D239/553 ,  C07D239/557

Abstract: A new intermediate is useful in the synthesis of elagolix. A process for obtaining the intermediate includes reacting a precursor with iodine monochloride in the presence of an organic solvent. A process for preparing elagolix makes use of the intermediate. The intermediate can be 3-((R)-2-(amino-2-phenylethyl)-1-(2-fluoro-6-trifluoromethylbenzyl)-5-iodo-6-methyl-1H-pyrimidine-2,4-dione or a salt thereof, such as a hydrochloride.

公开(公告)号：US20200239477A1

公开(公告)日：2020-07-30

申请号：US16754821

申请日：2018-10-11

Applicant: MOEHS IBERICA, S.L.

Inventor： Carles SÁNCHEZ CASALS ,  Alicia DOBARRO RODRÍGUEZ

IPC: C07D487/04 ,  C07D401/04 ,  C07D413/14

Abstract: The present invention relates to a method for preparing 3-[(4S)-8-bromo-1-methyl-6-(pyridin-2-yl)-4H-imidazo[1,2-a] [1,4]benzodiazepin-4-yl]-propionic acid methyl ester starting from 3-[(3S)-7-bromo-2-oxo-5-(pyridin-2-yl)-2,3-dihydro-1H-[1,4]-benzodiazepin-3-yl] propionic acid methyl ester, and novel compounds useful as intermediates in said method, i.e., (3S)-3-[7-bromo-2-(2,2-dimethoxypropylamino)-5-pyridin-2-yl-3H-benzo[e] [1,4]diazepin-3-yl]propionic acid methyl ester.