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1. 发明申请

US20120330014A1 METHOD FOR PRODUCING IMATINIB BASE 有权
标题翻译：生产图像基因的方法
公开(公告)号：US20120330014A1
公开(公告)日：2012-12-27
申请号：US13483750
申请日：2012-05-30
申请人： Hearan Suh , Sang Kyu Nam , Jong Sun Lee , Seung Ki Kim
发明人： Hearan Suh , Sang Kyu Nam , Jong Sun Lee , Seung Ki Kim
IPC分类号： C07D417/12 , C07D401/14
CPC分类号： C07D401/06 , C07D241/04 , C07D401/04
摘要： The present invention relates to a novel method for preparing an imatinib base, and more particularly to a method for preparing an imatinib base, which comprises reacting 4-(4-methyl-piperazinomethyl)-benzoic acid with a 2,2′-dibenzothiazolyl disulfide derivative in the presence of a phosphine derivative to prepare a novel thioester compound and preparing an imatinib base using the thioester compound as a reaction intermediate. In addition, the invention provides a novel thioester compound, which is used in the preparation of imatinib base, and a preparation method thereof. Ultimately, the invention provides a method of preparing the imatinib base in an economic manner and in high yield and purity and is expected to be used in the commercial production of large amounts of the imatinib base.
摘要翻译：本发明涉及一种制备伊马替尼碱的新方法，更具体地涉及一种制备伊马替尼碱的方法，该方法包括使4-（4-甲基 - 哌嗪基甲基） - 苯甲酸与2,2'-二苯并噻唑基二硫醚在膦膦衍生物的存在下制备新的硫酯化合物，并使用硫酯化合物作为反应中间体制备伊马替尼碱。另外，本发明提供了用于制备伊马替尼碱的新的硫酯化合物及其制备方法。最终，本发明提供了一种以经济的方式，高产率和纯度制备伊马替尼碱的方法，并且预期用于商业生产大量的伊马替尼碱。

2. 发明授权

US08563720B2 Method for producing imatinib base 有权
标题翻译：生产伊马替尼碱的方法
公开(公告)号：US08563720B2
公开(公告)日：2013-10-22
申请号：US13483750
申请日：2012-05-30
申请人： Hearan Suh , Sang Kyu Nam , Jong Sun Lee , Seung Ki Kim
发明人： Hearan Suh , Sang Kyu Nam , Jong Sun Lee , Seung Ki Kim
IPC分类号： C07D417/10
CPC分类号： C07D401/06 , C07D241/04 , C07D401/04
摘要： The present invention relates to a novel method for preparing an imatinib base, and more particularly to a method for preparing an imatinib base, which comprises reacting 4-(4-methyl-piperazinomethyl)-benzoic acid with a 2,2′-dibenzothiazolyl disulfide derivative in the presence of a phosphine derivative to prepare a novel thioester compound and preparing an imatinib base using the thioester compound as a reaction intermediate. In addition, the invention provides a novel thioester compound, which is used in the preparation of imatinib base, and a preparation method thereof. Ultimately, the invention provides a method of preparing the imatinib base in an economic manner and in high yield and purity and is expected to be used in the commercial production of large amounts of the imatinib base.
摘要翻译：本发明涉及一种制备伊马替尼碱的新方法，更具体地涉及一种制备伊马替尼碱的方法，该方法包括使4-（4-甲基 - 哌嗪基甲基） - 苯甲酸与2,2'-二苯并噻唑基二硫醚在膦膦衍生物的存在下制备新的硫酯化合物，并使用硫酯化合物作为反应中间体制备伊马替尼碱。另外，本发明提供了用于制备伊马替尼碱的新的硫酯化合物及其制备方法。最终，本发明提供了一种以经济的方式，高产率和纯度制备伊马替尼碱的方法，并且预期用于商业生产大量的伊马替尼碱。

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