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

Albert William Garofalo; Jacek Jerzy Jagodzinski; Andrei William Konradi; Raymond Anthony Ng; Christopher Michael Semko; Hing Leung Sham; Minghua Sun; Xiaocong Michael Ye

doi:10.1248/cpb.c110498

Notes

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

Albert William Garofalo, Jacek Jerzy Jagodzinski, Andrei William Konradi, Raymond Anthony Ng, Christopher Michael Semko, Hing Leung Sham, Minghua Sun, Xiaocong Michael Ye

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Keywords: intramolecular cycloaddition, nitrilimine, pyrazole, γ-secretase inhibitor

JOURNAL FREE ACCESS

2012 Volume 60 Issue 8 Pages 1063-1066

DOI https://doi.org/10.1248/cpb.c110498

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Abstract

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.

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