PROCESS FOR THE PREPARATION OF ACALABRUTINIB AND ITS INTERMEDIATES

• Main Authors: SINGH, Hemant Kumar, SANGHANI, Sunil, LAHIRI, Saswata, GUPTA, Chandan Kumar, SINGH, Govind, CABRI, Walter, GUPTA, Nitin, DHIMAN, Navdeep
• Format: Patent
• Language: English; French
• Published: 30.04.2020
• Subjects: CHEMISTRY; HETEROCYCLIC COMPOUNDS; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS

The present invention provides an improved and industrially viable process for the preparation of Acalabrutinib and its intermediates in high yield and eliminating the use of time-consuming purification process. The present invention also relates to the purification of (S)-4-(8-Amino-3-(pyrrolidin-2-yl)imidazo[1,5-alpyrazin-1-yl)-N-(pyridin-2-yl) benzamide, a key intermediate for the preparation of Acalabrutinib. Further present invention relates to new polymorphic form of Acalabrutinib. La présente invention concerne un procédé amélioré et industriellement viable pour la préparation d'Acalabrutinib et de ses intermédiaires à un rendement élevé et l'élimination de l'utilisation d'un procédé de purification chronophage. La présente invention concerne également la purification du (S)-4-(8-amino-3-(pyrrolidin-2-yl)imidazo[1,5-a]pyrazin-1-yl)-N-(pyridin-2-yl)benzamide, un intermédiaire clé pour la préparation de l'Acalabrutinib. La présente invention concerne en outre une nouvelle forme polymorphe de l'Acalabrutinib.