120686-00-2Relevant academic research and scientific papers
A process for the synthesis of intermediates in the preparation method of the huperzine-a
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Paragraph 0027; 0040; 0042; 0043, (2018/11/03)
The invention discloses a preparation method of an intermediate for synthesizing huperzine A. The preparation method comprises the following steps: substituting 3-bromine-6-methoxy-2-methyl pyridine taken as a raw material with N-bromosuccinimide so as to obtain a substitution product; carrying out a reaction on the substitution product and methyl acetoacetate and then carrying out ring closing reaction under the action of cuprous iodide so as to obtain 2-methoxy-6-hydroxy-7,8-dihydro-5-quinoline carboxylic methyl ester. According to the method provided by the invention, the synthesis reaction cost is low, so that the production cost is effectively lowered; the reaction conditions are moderate, so that the safety of operating personnel is ensured; a refining process is convenient and simple to operate; the intermediate obtained via the reaction is good in quality, high in yield and good in environmental friendliness.
METHOD OF PREPARING HUPERZINE A AND DERIVATIVES THEREOF
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Page/Page column 10; 7, (2009/10/06)
The present invention is related to the synthesis of huperzine A. The synthesis includes a variety of process steps that increase productivity, reduce safety concerns, and allow for increasing production of compounds of desired optical isomer. The inventive methods may encompass a single improved reaction step that may be incorporated into a known reaction process for synthesizing huperzine A or a derivative thereof to improve the overall reaction. The inventive methods also encompass complete synthesis methods for preparing huperzine A or a derivative thereof.
