PROCESS FOR CRYSTALLIZATION OF REVERSE TRANSCRIPTASE INHIBITOR USING ANTI-SOLVENT

PROBLEM TO BE SOLVED: To provide a Form I crystalline compound of (-)-6-chloro-4-cyclopropylethynyl-4-trifluoromethyl-1,4-dihydro-2H-3,1-benzoxazin-2-one, and a process of obtaining the crystalline compound.SOLUTION: A desired final crystal form, Form I, can be produced when using methanol or ethano...

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Bibliographische Detailangaben
Hauptverfasser:	CROCKER LOUIS S, CLARKE WILLIAM, KUKURA JOSEPH L II
Format:	Patent
Sprache:	eng ; jpn
Schlagworte:	BEER BIOCHEMISTRY CHEMISTRY COMPOSITIONS THEREOF CULTURE MEDIA ENZYMOLOGY HETEROCYCLIC COMPOUNDS HUMAN NECESSITIES HYGIENE MEDICAL OR VETERINARY SCIENCE METALLURGY MICROBIOLOGY MICROORGANISMS OR ENZYMES MUTATION OR GENETIC ENGINEERING ORGANIC CHEMISTRY PERFORMING OPERATIONS PHYSICAL OR CHEMICAL PROCESSES OR APPARATUS IN GENERAL PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES PROPAGATING, PRESERVING OR MAINTAINING MICROORGANISMS SEPARATION SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS SPIRITS TRANSPORTING VINEGAR WINE
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Beschreibung
Zusammenfassung:	PROBLEM TO BE SOLVED: To provide a Form I crystalline compound of (-)-6-chloro-4-cyclopropylethynyl-4-trifluoromethyl-1,4-dihydro-2H-3,1-benzoxazin-2-one, and a process of obtaining the crystalline compound.SOLUTION: A desired final crystal form, Form I, can be produced when using methanol or ethanol from a solvent and anti-solvent system. Form II is isolated from 2-propanol and can be converted to a desired crystal form at low drying temperatures, such as temperatures from about 40°C to about 50°C. 【課題】（−）−６−クロロ−４−シクロプロピルエチニル−４−トリフルオロメチル−１，４−ジヒドロ−２Ｈ−３，１−ベンゾオキサジン−２−オンのＩ型結晶化合物、および該結晶化合物の取得方法を提供する。【解決手段】溶媒・逆溶媒系から、所望の最終結晶形態であるＩ型を、メタノールまたはエタノールを使用した場合に得ることができる。ＩＩ型は、２−プロパノールから単離され、低い乾燥温度（例えば、約４０℃から約５０℃の温度）で所望の結晶形態に変換することができる。【選択図】なし