Development of the Route of Manufacture of an Oral H1− H3 Antagonist

G Bret, SJ Harling, K Herbal, N Langlade…

Index: Harling, Sandra J.; Herbal, Karim; Langlade, Nathalie; Sanganee, Mahesh; Strachan, John B.; Turner, Peter G.; Whiting, Matthew P.; Bret, Guillaume; Loft, Mike; Negus, Alan; Shanahan, Steve Organic Process Research and Development, 2011 , vol. 15, # 1 p. 112 - 122

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Citation Number: 9

Abstract

There were a number of issues associated with this synthesis which precluded its use as the long-term route of manufacture. Use of p-iodophenol generates iodine-containing waste streams and associated high disposal costs. The use of a BOC protecting group for the piperidone raises issues of thermal stability and the generation of isobutylene as a byproduct. The cryogenic temperature and low yield for the Grignard reaction was unsatisfactory and the resulting ...

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