The Chemical Development of the Commercial Route to Sildenafil: A Case History

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 chemica...

Full description

Saved in:

Bibliographic Details
Published in:	Organic process research & development Vol. 4; no. 1; pp. 17 - 22
Main Authors:	Dale, David J, Dunn, Peter J, Golightly, Clare, Hughes, Michael L, Levett, Philip C, Pearce, Andrew K, Searle, Patricia M, Ward, Gordon, Wood, Albert S
Format:	Journal Article
Language:	English
Published:	American Chemical Society 01-01-2000
Online Access:	Get full text
Tags:	Add Tag No Tags, Be the first to tag this record!

Description
Summary:	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.
ISSN:	1083-6160 1520-586X
DOI:	10.1021/op9900683