- A S - west reaches anchors the sandbank and its salt synthesis method
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The invention discloses a synthetic method for S-dapoxetine. The synthetic method comprises the following steps: (1) resolving 1-phenyl-3-(naphthyl-1-oxy)propylamine for at least once with a resolving agent to obtain a resolved mixed system; (2) separating the resolved mixed system to obtain S-1-phenyl-3-(naphthyl-1-oxy)propylamine, and recycling mother liquor; (3) performing methylation on the S-1-phenyl-3-(naphthyl-1-oxy)propylamine to obtain S-dapoxetine. Compared with the conventional industrial production method, residual intermediate (R)-phenyl-3-(naphthyl-1-oxy)propylamine in the resolved mother liquor is firstly recycled on the basis of the prior art, then resolved again through D-(-) tartaric acid after racemization, and recycled, so that the yield is increased, the product waste is avoided, and the economic benefits are improved.
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- A west reaches anchors the sandbank and method for industrial preparation of the intermediates
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The invention relates to an industrial preparation method of apoxetine and an intermediate of apoxetine. According to the method, methylation, condensation and salt forming reaction are carried out on 3-amino-3-phenyl propanol serving as a starting raw material to obtain the apoxetine and the intermediate of apoxetine. The method overcomes the deficiencies in the prior art, comprises simple and short reaction steps and is convenient and fast to operate and suitable for industrial production; moreover, the raw materials are simple and easily available.
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Paragraph 0068-0073
(2016/10/08)
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