Solid-state properties and crystallization behavior of PHA-739521 polymorphs.
PHA-739521 is an experimental compound that exhibits polymorphism. The two anhydrous crystal forms, I and II, are characterized using powder X-ray diffractometry, thermal analyses, moisture sorption gravimetry. Both Forms I and II are non-hygroscopic and are stable to compaction pressure. The melting temperature is about 152 degrees C for Form I and 168 degrees C for Form II. Forms I and II are enantiotropically related where Form I is more stable below a transition temperature of approximately 70 degrees C. Crystallization behavior of this compound from solutions and during heating is also studied. Information obtained is used to design an appropriate crystallization process to successfully manufacture desired polymorph at large scale.
Sun
Changquan Calvin
CC
Pfizer Global Research and Development, 7000 Portage Road, Portage, MI 49001, USA. ccsun@amgen.com
D002152:Calorimetry, Differential Scanning; D011232:Chemical Precipitation; D002626:Chemistry, Pharmaceutical; D019245:Compressive Strength; D003460:Crystallization; D018360:Crystallography, X-Ray; D011720:Pyrazoles / Q000737:chemistry*; D012995:Solubility; D013237:Stereoisomerism; D013449:Sulfonamides / Q000737:chemistry*; D013678:Technology, Pharmaceutical; D013816:Thermodynamics; D044366:Transition Temperature; D014867:Water / Q000737:chemistry; D017155:Wettability
C515247:PHA-739521; D011720:Pyrazoles; D013449:Sulfonamides; D014867:Water