Crystallization Control and Physicochemical Properties of Polymorphic Forms of the Factor Xa Inhibitor KFA-1982

详细信息    查看全文

• 作者：Hideki Takeuchi ; Koji Kamata ; Eiichi Tsuji ; Harunobu Mukaiyama ; Yuichiro Kai ; Kenji Yokoyama ; Kazumichi Jo ; Katsuhide Terada
• 刊名：Organic Process Research & Development
• 出版年：2012
• 出版时间：April 20, 2012
• 年：2012
• 卷：16
• 期：4
• 页码：647-653
• 全文大小：313K
• 年卷期：v.16,no.4(April 20, 2012)
• ISSN：1520-586X

文摘

Many polymorphs of KFA-1982, an orally active factor Xa (fXa) inhibitor, have been identified and their physicochemical properties have been investigated. Form B was selected as the oral API form because of its superior stability and solubility characteristics. Crystallization conditions for form B were thoroughly investigated including the role of water in hydrate formation and the use of antisolvents and supersaturation in polymorph control.