PROCESSES FOR PREPARATION OF (3S,4R)-3-ETHYL-4-(3H-IMIDAZO[1,2-a]PYRROLO[2,3-e]-PYRAZIN-8-YL)-N-(2,2,2-TRIFLUOROETHYL)PYRROLIDINE-1-CARBOXAMIDE AND SOLID STATE FORMS THEREOF

• Main Authors: AHMAD Y SHEIKH, MICHAEL J ROZEMA, THOMAS B BORCHARDT, PETER T MAYER, BEN KLUENDER, MATHEW M MULHERN, AYMAN ALLIAN, MOHAMED-ESLAM F MOHAMED, LAKSHMI BHAGAVATULA, JAYANTHY JAYANTH, AHMED A OTHMAN, PATRICK J MARROUM, FREDRIK LARS NORDSTROM
• Format: Patent
• Language: English; Japanese
• Published: 18.02.2021
• Subjects: ACYCLIC OR CARBOCYCLIC COMPOUNDS; CHEMICAL OR PHYSICAL PROCESSES, e.g. CATALYSIS OR COLLOIDCHEMISTRY; CHEMISTRY; HETEROCYCLIC COMPOUNDS; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PERFORMING OPERATIONS; PHYSICAL OR CHEMICAL PROCESSES OR APPARATUS IN GENERAL; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS; THEIR RELEVANT APPARATUS; TRANSPORTING

To provide processes for preparing (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide, solid state forms thereof, and corresponding pharmaceutical compositions, methods of treatment (including treatment of rheumatoid arthritis), kits, methods of synthesis, and products-by-process.SOLUTION: A process for preparing a crystalline hydrate comprises: dissolving (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide in a solvent or solvent mixture; and initiating crystallization to provide the crystalline hydrate.SELECTED DRAWING: Figure 1A 【課題】（３Ｓ，４Ｒ）−３−エチル−４−（３Ｈ−イミダゾ［１，２−ａ］ピロロ［２，３−ｅ］ピラジン−８−イル）−Ｎ−（２，２，２−トリフルオロエチル）ピロリジン−１−カルボキサミド、それの固体型、および相当する医薬組成物の製造方法、治療方法（関節リウマチの治療など）、キット、合成方法、ならびにプロダクト・バイ・プロセスの提供。【解決手段】（３Ｓ，４Ｒ）−３−エチル−４−（３Ｈ−イミダゾ［１，２−ａ］ピロロ［２，３−ｅ］ピラジン−８−イル）−Ｎ−（２，２，２−トリフルオロエチル）ピロリジン−１−カルボキサミドを溶媒もしくは溶媒の混合物に溶解させること；および結晶化を開始して、前記結晶性水和物を提供することを含む、結晶性水和物の製造方法。【選択図】図１Ａ