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Synthesis 2010(20): 3429-3432  
DOI: 10.1055/s-0030-1258212
PAPER
© Georg Thieme Verlag Stuttgart ˙ New York

A Facile and Green Synthesis of a Naphthyridine Derivative: A Novel Hedgehog Pathway Modulator

Wen-Chung Shieh*, Song Xue, Joe McKenna, Kapa Prasad, Mahavir Prashad
Chemical and Analytical Development, Novartis Pharmaceuticals Corporation, East Hanover, NJ 07936, USA
Fax: +1(973)7817566; e-Mail: wen.shieh@novartis.com;
Further Information

Publication History

Received 6 May 2010
Publication Date:
13 August 2010 (online)

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Abstract

A green and highly efficient synthesis of a naphthyridine derivative, a novel hedgehog pathway modulator, in high yield and purity from inexpensive starting materials is described. The key step involves an acid-promoted aryl amination reaction of aniline with naphthyridine halides.

Key words

aryl amination - acid-promoted coupling - green chemistry - naphthyridine - pyridine cyclization

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