MACROLIDE SYNTHESIS PROCESS

• Main Authors: WENNESHEIMER HEINZ JOERG, FLEISCHHAUER KERSTIN, WARRASS RALF, HU GUIXIAN, BLATTER FRITZ, BRINK MONIKA, NIEDERMANN HANS PETER, BRENNER MEINRAD, RAGER TIMO, SCHWEISEL TANJA, VEIT STEPHAN
• Format: Patent
• Language: English; Korean
• Published: 12.06.2014
• Subjects: CHEMISTRY; DERIVATIVES THEREOF; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; NUCLEIC ACIDS; NUCLEOSIDES; NUCLEOTIDES; ORGANIC CHEMISTRY; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS; SUGARS

본 발명은 마크롤라이드의 제조 방법 및, 특히 선택적으로 치환된 20, 23-디피페리디닐-5-O-마이카미노실-타일로놀라이드 및 이의 유도체의 제조 방법뿐만 아니라, 약제 제조를 위한 마크롤라이드의 용도, 마크롤라이드를 이용한 치료 방법 및 특히, 마크롤라이드 제조에 사용될 수 있는 중간체 제조 방법에 관한 것이다. Described are methods for making macrolides, and, in particular, a method for making optionally substituted 20,23-dipiperidinyl-5-O-mycaminosyl-tylonolide and derivatives thereof, as well as uses of macrolides to make medicaments, methods of treatment using macrolides, and methods for making intermediates that, among other uses, may be used to make macrolides. Also described are solvated and non-solvated crystalline forms of 20,23-dipiperidinyl-5-O-mycaminosyl-tylonolide, as well as methods for making such crystalline forms, medicaments comprising (or derived from) such crystalline forms, methods for making medicaments comprising (or derived from) such crystalline forms, methods of treatment using such crystalline forms, and kits comprising such crystalline forms.