브로모도메인 억제제의 제조 방법

• Main Authors: RUDA ANTONIO MARIA, TRAVERSE JOHN FITZGERALD, YONG KELVIN HIN YEONG, PHILP STEVEN, ALITE HEKLA, MOSELEY JONATHAN, FERRETTI ANTONIO CHRISTIAN, PRIMER DAVID
• Format: Patent
• Language: Korean
• Published: 24.05.2021
• Subjects: ACYCLIC OR CARBOCYCLIC COMPOUNDS; ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAININGELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN,SULFUR, SELENIUM OR TELLURIUM; 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

본 발명은 브로모도메인 억제제인 화합물 1 (그의 결정질 형태, 무정형 형태, 용매화물 및 수화물을 포함함)의 합성 및 정제 공정을 제공한다.　 본 개시내용의 실시양태는 고도로 순수한 최종 생성물을 생성하는 확장가능한 방법을 제공하는 화합물 1의 화학적 합성 경로에 관한 것이다.　 추가 실시양태는 포름산 및 물로부터 결정화에 의해 화합물 1의 가장 안정한 다형체를 단리하는 방법에 관한 것이다. The present invention provides processes of synthesis and purification of a bromodomain inhibitor, Compound 1, which compound includes crystalline forms, amorphous forms, solvates, and hydrates thereof. Embodiments of the disclosure relate to chemical synthesis routes of Compound 1 that provide a scalable method that results in highly pure final product. A further embodiment relates to methods to isolate the most stable polymorph of Compound 1 by crystallization from formic acid and water.