公开(公告)号：KR100799821B1

公开(公告)日：2008-01-31

申请号：KR1020070011556

申请日：2007-02-05

Applicant: 동화약품주식회사

Inventor： 오윤석 ,  임재경 ,  신동혁 ,  성승규 ,  이상호 ,  이학수 ,  조은희 ,  유제만

IPC: C07D401/14

CPC classification number: C07D401/04

Abstract: An imatinib camsylate is provided to be more rapidly absorbed and show higher absorption concentration and excellent solubility in water than those of a commercially available imatinib mesylate in the pharmacokinetic aspect. An imatinib camsylate is represented by the formula(1), wherein HX is D-(+)-camphorsulfonic acid, L-(-)-camphorsulfonic acid or D,L-(±)-camphorsulfonic acid. A method for preparing the imatinib camsylate comprises the steps of: (a) dissolving an imatinib represented by the formula(2) in an organic solvent; (b) dissolving one acid represented by the formula(3) or (4), or an acid which is a mixture of the formula(3) and the formula(4) in a ratio of 1:1 in an organic solvent or adding the acid as it is to the reaction solution obtained from the step(a) to prepare a mixture; (c) filtering a solid extracted by agitating the mixture to form an acid addition salt; and (d) after dissolving the acid addition salt in an organic solvent and re-filtering it to extract crystal, purifying the crystal.

Abstract translation: 提供了一种伊马替尼樟脑磺酸盐以在药代动力学方面比在商业上可获得的甲磺酸伊马替尼的那些更快速地吸收并显示更高的吸收浓度和在水中的优异的溶解性。 伊马替尼樟脑磺酸盐由式（1）表示，其中HX是D - （+） - 樟脑磺酸，L - （ - ） - 樟脑磺酸或D，L-（±） - 樟脑磺酸。 制备伊马替尼樟脑磺酸盐的方法包括以下步骤：（a）将由式（2）表示的伊马替尼溶解在有机溶剂中; （b）在有机溶剂中溶解由式（3）或（4）表示的一种酸或以式（3）和式（4）的混合物形式的酸的比例为1:1，或者将 将酸从原来的步骤（a）获得的反应溶液制备成混合物; （c）过滤通过搅拌混合物提取的固体形成酸加成盐; 和（d）将酸加成盐溶解在有机溶剂中并对其进行再过滤以萃取晶体，纯化晶体。