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ChemInform Abstract: Pilot-Scale Synthesis of a Novel Non-Xanthine Adenosine A1 Receptor Antagonist. 1,3-Dipolar Cycloaddition of Pyridine N-Imine to an Acetylene.

✍ Scribed by A. ZANKA; N. HASHIMOTO; R. UEMATSU; T. OKAMOTO

Publisher: John Wiley and Sons
Year: 2010
Weight: 34 KB
Volume: 30
Category: Article
ISSN: 0931-7597
DOI: 10.1002/chin.199905120

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✦ Synopsis

Pilot-Scale Synthesis of a Novel Non-Xanthine Adenosine A 1 Receptor Antagonist. 1,3-Dipolar Cycloaddition of Pyridine N-Imine to an Acetylene.

-A new, concise and efficient large scale procedure for the preparation of title compound FK838 (VII) is developed. It is based on a detailed investigation of the 1,3-dipolar cycloaddition of pyridine N-imine (II) to acetylene (I) which allows the smooth isolation of key intermediate (III) in remarkably high yield and quality. All work-up and purification steps are based on extraction and crystallization. The procedure presented is successfully applied to a pilot plant to afford more than 200 kg of (VII) for pharmaceutical and toxicological evaluation.

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