Chen Xin-li, He Yi, Li Jue
2015
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Journal
Chinese Journal of Medicinal Chemistry
Abstract
To synthesize two important impurities of almotriptan malate named related substance G and related substance I,related substance G was synthesized via the direct oxidation of almotriptan by m CPBA. Related substance I was synthesized from ethyl 4-aminobenzoate via diazotization / reduction,Fisher cyclization,reduction and coupling with almotriptan under 1 mol·L- 1HCl. Related substance G was successfully synthesized by a novel route with a higher yield and more simplified operation than literature. At the same time,related substance I was synthesized for the first time. The designed route has the advantages of mild reaction conditions,cheap and normol reagents and simple operation. The detailed data of related substance G and related substance I was reported for the first time.