TY - JOUR
AU1 - Laha, Joydev K.
AU2 - Gulati, Upma
AU3 - Saima,
AU4 - Gupta, Anjali
AU5 - Indurthi, Harish Kumar
AB - An improved, gram-scale synthesis of the blockbuster drug sildenafil, used for the treatment of male erectile dysfunction, has been developed. Unlike the previous literature, the current method demonstrates the use of arylacetic acid as an acyl source, a cheap oxidant K2S2O8, and water as the reaction medium in the key step of pyrrazolo[4,3-d]pyrimidin-7-one ring formation. As well as being a green and benign approach, the current method reduces the cost by half compared to our previous strategy. In addition, the general relevance of the method has been demonstrated in the synthesis of a variety of quinazolinone and benzothiazole derivatives with excellent functional group tolerance.
TI - Improved, gram-scale synthesis of sildenafil in water using arylacetic acid as the acyl source in the pyrazolo[4,3-d]pyrimidin-7-one ring formation
JF - NJC: New Journal of Chemistry
DO - 10.1039/d0nj01236j
DA - 2021-02-10
UR - https://www.deepdyve.com/lp/royal-society-of-chemistry/improved-gram-scale-synthesis-of-sildenafil-in-water-using-arylacetic-IQGpCPHJYd
SP - 2643
EP - 2648
VL - 45
IS - 5
DP - DeepDyve
ER -