期刊
NEW JOURNAL OF CHEMISTRY
卷 45, 期 5, 页码 2643-2648出版社
ROYAL SOC CHEMISTRY
DOI: 10.1039/d0nj01236j
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资金
- NIPER
- CSIR, New Delhi
- S. A. S. Nagar
An improved gram-scale synthesis of sildenafil has been developed using arylacetic acid, a cheap oxidant, and water, reducing costs by half and showing broad application in the synthesis of related derivatives.
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.
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