Synthesis of Novel Tetrahydro-1H-pyrazolo[4,3-c]pyridines via Intramolecular Nitrilimine Cycloaddition

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The preparation of novel tetrahydro-1H-pyrazolo[4,3-c]pyridines is reported. Pivotal to the synthesis of these compounds was the development of mild reaction conditions to generate a highly functionalized nitrilimine capable of undergoing an intramolecular cycloaddition with a tethered alkyne. The desired cycloadduct was formed as an equal mixture of diastereomers.
公益社団法人　日本薬学会の論文