The development of an effective synthetic route of rilpivirine

Abstract Background Rilpivirine (RPV) was approved by the U.S. FDA (Food and Drug Administration) in 2011 to treat individuals infected with human immunodeficiency virus 1 (HIV-1). Significantly, rilpivirine is three fold more potent than etravirine. Once-daily, it used a low oral dose (25 mg/tablet), decreasing drug administration bringing better choice patients. However, there are many shortcomings existing synthesis route of RPV, such as high cost, prolonged reaction time yield (18.5%). Results This article describes our efforts develop an efficient practical microwave-promoted method synthesize using less toxic organic reagents boiling solvents. The last step's decreased from 69 h 90 min through this optimized synthetic procedure, overall improved 18.5 21%. In addition, intermediate 3 increased 52 62% compared original patent. Conclusion Overall, series process optimization, we have developed rilpivirine, which easy scale higher shorter time.