期刊
ORGANIC PROCESS RESEARCH & DEVELOPMENT
卷 4, 期 1, 页码 17-22出版社
AMER CHEMICAL SOC
DOI: 10.1021/op9900683
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This paper is a case history of the chemical development of sildenafil which covers various aspects of work in chemical development namely: route selection, scale-up issues, the development of an efficient synthesis with high throughput, process-safety, and environmental issues. Interesting chemical points include improved methods of preparing pyrazolo[4,3-d]pyrimidines and the unusual isolation of an intermediate as its double salt (10). The potential dangers of nitrating pyrazole-5-carboxylic acids which are activated to a decarboxylation reaction are discussed.
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