- Preparation method of clopidogrel hydrogen sulfate and intermediate N-(2-thiopheneethyl) methyleneimine of clopidogrel hydrogen sulfate
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The invention discloses a preparation method of clopidogrel hydrogen sulfate and an intermediate N-(2-thiophene ethyl) methyleneamine of the clopidogrel hydrogen sulfate. The synthesis method of the intermediate comprises the step of carrying out an Eschweiler-Clarke methylation reaction by taking 2-thiophene ethylamine and paraformaldehyde as raw materials to obtain the N-(2-thiophene ethyl) methyleneamine. The invention also provides a method for preparing clopidogrel hydrogen sulfate. According to the synthesis method provided by the invention, the required solid product (N-(2-thiopheneethyl) methyleneimine) is synthesized in one step, the synthesis method is simple, the qualified solid compound is directly obtained, the time and the raw material cost are saved, the storage and the transportation are convenient, the purity is good, the yield is high, and the synthesis method is suitable for industrial production.
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Paragraph 0109; 0114
(2021/05/08)
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- A PROCESS FOR THE PREPARATION OF S-CLOPIDOGREL
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A process for the preparation of (S) - Clopidogrel free base or a pharmaceutically acceptable salt thereof by the racemization of the undesired (R) - Clopidogrel in the presence of a suitable base followed by resolution with camphor sulfonate salt and further treatment with an inorganic acid to yield the title compound.
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Page/Page column 12
(2010/05/13)
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