Improvement in the Synthesis Process of Antifungal Bulk Drug Posaconazole
Objective:To design a new synthetic process route of posaconazole suitable for industrial production.Methods:4-(4-(4-nitrophenyl)-1-piperazinyl)phenol was used as starting material to react with four hydroxyl protective group reagents,and then posaconazole was obtained by nitro-reduction,conden-sation,cyclization and reduction.Results:Four reagents including acetyl chloride,3,4-dihydro-2H-pyran,triphenylchloromethane and benzyl chloride were used as hydroxyl protective group,and the total reaction yields were 46.93%,40.41%,36.73%,and 20.17%,respectively.Conclusion:The synthesis process of posaconazole using acetyl chloride as hydroxyl protective group can avoid the introduction of impurities con-taining benzene or pyran rings,and ensure the product quality from the source.This process has the advan-tages of short route,high total yield and controllable quality,laying a good foundation for industrial produc-tion.
posaconazolesynthesisacetyl chloridehydroxyl protective group
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