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Paliperidone intermediate and method for producing paliperidone using the same

机译:帕潘立酮中间体和使用该中间体生产帕潘立酮的方法

摘要

Disclosed are novel intermediates of paliperidone which are used as a therapeutic agent for schizophrenia, and to a method for producing paliperidone using the same. The intermediates are a compound represented by chemical formula 3 and a compound represented by chemical formula 5. The method for producing paliperidone comprises a step of conducting a reaction of a compound represented by chemical formula 5 and an acid compound. In the chemical formulas 3 and 5, R is a silyl group, a hydrocarbon group having 1-20 carbon atoms, a protecting group represented by -R_1OR_2 or -R_1SR_2, or a protecting group represented by -C(=O)R_2. In particular, R_1 is a methylene group or a carbonyl group, and R_2 is a substituted or unsubstituted alkyl group, an aryl group, or an alkylaryl group, wherein R_1 and R_2 can bond to each other to form a ring.
机译:公开了用作精神分裂症治疗剂的帕潘立酮的新型中间体,以及使用该中间体生产帕潘立酮的方法。中间体是化学式3表示的化合物和化学式5表示的化合物。帕潘立酮的制造方法包括使化学式5表示的化合物与酸化合物反应的步骤。在化学式3和5中,R为甲硅烷基,具有1-20个碳原子的烃基,由-R_1OR_2或-R_1SR_2表示的保护基或由-C(= O)R_2表示的保护基。特别地,R_1是亚甲基或羰基,并且R_2是取代或未取代的烷基,芳基或烷基芳基,其中R_1和R_2可以彼此键合以形成环。

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