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1. 发明申请

US20110275805A1 METHOD FOR PREPARING LINEZOLID AND INTERMEDIATES THEREOF 有权
标题翻译：制备线粒体的方法及其中间体
公开(公告)号：US20110275805A1
公开(公告)日：2011-11-10
申请号：US13144242
申请日：2010-01-08
申请人： Ping Wang , Qiangbiao Pan , Yangzhou Li , Daoliang Zheng
发明人： Ping Wang , Qiangbiao Pan , Yangzhou Li , Daoliang Zheng
IPC分类号： C07D413/10 , C07C211/15
CPC分类号： C07D263/20
摘要： A method for preparing the linezolid (compound 1), which comprises the steps of: (1) carrying out the debenzyl reaction of compound 4 in solvent, to obtain the compound 5 or its acetate; (2) carrying out the acetylation reaction in the amino of the compound 5 or its acetate obtained in step (1) in solvent to obtain the compound 1. The intermediates to prepare the compound 1 and the acetate of compound 5. The present preparation method is easy to obtain the chiral materials and the chiral materials are cheap, the process and the post treatment are simple, the intermediate products and the end product are easy to be purified, the total yield is high, their purities are also high, this preparation method is easy to be used in the industry manufacture.
摘要翻译：一种制备利奈唑胺（化合物1）的方法，包括以下步骤：（1）在溶剂中进行化合物4的脱苄基反应，得到化合物5或其乙酸酯; （2）在溶剂中在步骤（1）中得到的化合物5或其乙酸的氨基进行乙酰化反应，得到化合物1.制备化合物1和化合物5的乙酸酯的中间体。本制备方法手性材料易于获得，手性材料便宜，工艺和后处理简单，中间产品和最终产品易于纯化，总产率高，纯度高，该制剂方法易于在工业制造中使用。

2. 发明授权

US08658789B2 Method for preparing linezolid and intermediates thereof 有权
标题翻译：制备利奈唑胺的方法及其中间体
公开(公告)号：US08658789B2
公开(公告)日：2014-02-25
申请号：US13144242
申请日：2010-01-08
申请人： Ping Wang , Qiangbiao Pan , Yangzhou Li , Daoliang Zheng
发明人： Ping Wang , Qiangbiao Pan , Yangzhou Li , Daoliang Zheng
IPC分类号： C07D413/10 , C07C211/01
CPC分类号： C07D263/20
摘要： A method for preparing the linezolid (compound 1), which comprises the steps of: (1) carrying out the debenzyl reaction of compound 4 in solvent, to obtain the compound 5 or its acetic acid salt; (2) carrying out the acetylation reaction in the amino of the compound 5 or its acetic acid salt obtained in step (1) in solvent to obtain the compound 1. The intermediates to prepare the compound 1 and the acetic acid salt of compound 5. The present preparation method is easy to obtain the chiral materials and the chiral materials are cheap, the process and the post treatment are simple, the intermediate products and the end product are easy to be purified, the total yield is high, their purities are also high, this preparation method is easy to be used in the industry manufacture.
摘要翻译：一种制备利奈唑胺（化合物1）的方法，包括以下步骤：（1）在溶剂中进行化合物4的脱苄基反应，得到化合物5或其乙酸盐; （2）在溶剂中在步骤（1）中得到的化合物5或其乙酸盐的氨基中进行乙酰化反应，得到化合物1.制备化合物1和化合物5的乙酸盐的中间体。本发明的制备方法易于获得手性物质，手性物料便宜，工艺和后处理简单，中间产物和最终产品容易纯化，总产率高，纯度也高高，这种制备方法在工业制造中很容易使用。

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