application | 6, 7-dihydro-5H-pyrrolo [3,4-b] pyridine Chinese alias 6, 7-dihydro-5H-pyrrolo [3,4,6] pyridine, pyrrolo pyridine ring compound is an important pharmaceutical intermediate, it is mainly used to synthesize moxifloxacin (Moxifloxacin), a new fluoroquinolone drug. At present, the market demand is large and the price is relatively high. Scientists from various countries have done a lot of research on its synthesis. In recent years, the clinical dosage of fluoroquinolones has exceeded that of penicillin. It is low in price, well absorbed, can be taken orally and injected, and can be quickly distributed to various tissues. As a new fluoroquinolone drug, moxifloxacin has received extensive attention from scientists. |
preparation | using pyridine 2, 3-dicarboxylate as raw material, first esterify to generate dimethyl pyridine dicarboxylate, and then use a mixed reagent composed of sodium borohydride and anhydrous calcium chloride to reduce the corresponding methyl ester. The reaction product can directly carry out the next chlorination reaction without purification. The chlorination product uses acetonitrile as the solvent, using anhydrous potassium carbonate as a base, the cyclization product 6, 7-dihydro-pyrrolo [3, 4-b] pyridine can be obtained by reacting at room temperature. The method has novel design, mild reaction conditions and simple reaction treatment, which is especially suitable for industrialization and enriches the synthesis methods of pyrrolo pyridine ring compounds. 6, 7-dihydro-5H-pyrrolo [3,4-b] pyridine preparation roadmap is as follows: fig. 1 6, 7-dihydro-5H-pyrrolo [3,4-b] pyridine preparation roadmap |