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Synthetic technology of molidustat
Author(s): 
Pages: 411-414
Year: Issue:  4
Journal: World Phytomedicines

Keyword:  molidustatrenal anemiaorganic synthesis;
Abstract: Objective To study the synthetic technology of molidustat. Methods 4,6-Dichloro pyrimidine was used as starting material to synthesize intermediate 4-(6-hydrazine pyrimidine-4-yl)morpholine(2) by introducing morpholine and hydrazine group successively. 1H-1,2,3-Triazole and ethyl bromoacetate were used as starting materials to synthesize intermediate(Z/E)-3-(dimethyl amine)-2-(1H-1,2,3-triazole-1-yl)ethyl acrylate(4) by hydrocarbylation and condensation reactions. Molidustat(5) was synthesized by cyclization reaction with intermediates 2 and 4, and sodium of molidustat(6) was synthesized by saltforming reaction. Results The target compound and its sodium were synthesized and characterized by 1H-NMR and MS. The total yield of this synthetic route was 31.5%. Conclusion The synthetic process with simple operation and simplified method is applicable to pilot manufacture, and has a good application prospect.
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