5-{8-[(3R)-4-ACETYL-3-METHYLPIPERAZIN-1-YL]-6-MORPHOLIN-4-YL-9-(2,2,2-TRIFLUOROETHYL)-9H-PURIN-2-YL}PYRIMIDINE-2- AMINE AND NOVEL CRYSTAL OF PHARMACOLOGICALLY ACCEPTABLE SALT THEREOF, AND METHOD FOR PRODUCING SAID CRYSTAL
5-{8-[(3R)-4-acetyl-3-methylpiperazin-1-yl]- 6-morpholin-4-yl-9-(2,2,2-trifluoroethyl)-9H-purin-2- yl}pyrimidine-2-amine which has properties suitable for the production thereof on an industrial scale, and a novel crystal of a pharmacologically acceptable salt thereof and a method for producing the crystal. 5-{8-[(3R)-4-acetyl-3-methylpiperazin-1-yl]-6-morpholin-4- yl-9-(2,2,2-trifluoroethyl)-9H-purin-2-yl}pyrimidine-2- amine and a crystal of a pharmacologically acceptable salt thereof provided by the present invention exhibit a poor hygroscopic property. Therefore, the compound and the crystal have excellent storage stability, can be synthesized suitably in a large quantity on an industrial scale, and have good physical properties for use as an active ingredient for a medicine. By employing a method for producing the crystal provided by the present invention, it becomes possible to produce a single crystal having a specific level of quality with good reproducibility and it also becomes possible to steadily supply the crystal as a crystal of an active ingredient that can be used for the production of a medicine.本發明之課題係提供具有適合工業生產性質的5-{8-[(3R)-4-乙醯基-3-甲基哌-1-基]-6-啉-4-基-9-(2,2,2-三氟乙基)-9H-嘌呤-2-基}嘧啶-2-胺、及其藥理容許鹽之新穎結晶、及其製造方法。藉由本發明所提供之5-{8-[(3R)-4-乙醯基-3-甲基哌-1-基]-6-啉-4-基-9-(2,2,2-三氟乙基)-9H-嘌呤-2-基}嘧啶-2-胺、及其藥理容許鹽之結晶,因難以呈現吸濕性,故保存安定性優異,適合於工業生產中的大量合成,具有作為醫藥品之原藥的良好物性。又,使用依據本發明所提供的結晶之製造方法時,具有一定品質的單一結晶為再現性良好地被獲得,安定地供給作為醫藥製造所使用的原藥之結晶成為可能。
