☆ 4.6 Article

Selection and Development of the Manufacturing Route for EP1 Antagonist GSK269984B

ORGANIC PROCESS RESEARCH & DEVELOPMENT (2010)

期刊

ORGANIC PROCESS RESEARCH & DEVELOPMENT

卷 14, 期 4, 页码 820-831

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AMER CHEMICAL SOC

DOI: 10.1021/op100072y

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Chemistry, Applied Chemistry, Organic

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A potential manufacturing route for the EP1 antagonist GSK269984B was developed. Four synthetic approaches were examined, and a successful realisation of each is presented. The rationale supporting selection of the preferred route is discussed. This route utilised a phenolic aldol reaction as the key step and relied on selective hydrogenolysis to reduce an intermediate diarylmethanol. Further optimisation of the selected route is presented, delivering GSK269984B in three stages and 46% overall yield from readily available starting materials.

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