Methods for producing beraprost and its derivatives

• Main Authors: WALSH DAVID A, PENMASTA RAJU, BATRA HITESH, TULADHAR SUDERSAN M, TUMMALA SRI H
• Format: Patent
• Language: Chinese; English
• Published: 19.04.2017
• Subjects: CHEMISTRY; HETEROCYCLIC COMPOUNDS; METALLURGY; ORGANIC CHEMISTRY

The present invention is directed to methods for preparing Beraprost and novel synthetic intermediates for Beraprost. In one aspect, a process is provided to produce a pharmaceutical compound represented by the general Formula (I) via a radical cyclization route. The process is completed in fewer steps than the known synthetic methods and may be conducted to prepare commercially useful quantities. In another aspect, synthetic methods are provided for producing Beraprost and its derivatives,, which are stereoselective, efficient, scalable and economical. In another aspect, substantially isomerically pure compounds and intermediates are produced by the above processes. 本发明涉及制备贝前列素和贝前列素的新合成中间体的方法。在个方面中，提供了通过自由基环化途径产生通式(I)所述的药物化合物的方法。该方法以比已知合成方法更少的步骤完成并且可进行以制备商业上可用的量。在另个方面中，提供了合成方法来产生贝前列素及其衍生物，其是立体选择性的、高效的、可放大的和经济的。在另个方面中，通过上述方法产生基本异构纯的化合物和中间体。