| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1365011 | Bioorganic & Medicinal Chemistry Letters | 2008 | 6 Pages |
Abstract
3-(Benzimidazol-2-yl)-pyridine-2-one-based ATP competitive inhibitors of Insulin-like Growth Factor 1 Kinase (IGF-IR) were optimized for reduced Cyp3A4 inhibition and improved oral exposure. The use of malonate as methyl anion synthon via SNAr reaction and double decarboxylation under mild conditions is demonstrated.
Graphical abstract3-(Benzimidazol-2-yl)-pyridine-2-one-based ATP competitive inhibitors of Insulin-like Growth Factor 1 Kinase (IGF-IR) were optimized for reduced Cyp3A4 inhibition and improved oral exposure. The use of malonate as methyl anion synthon via SNAr reaction and double decarboxylation under mild conditions is demonstrated.Figure optionsDownload full-size imageDownload as PowerPoint slide
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Kurt Zimmermann, Mark D. Wittman, Mark G. Saulnier, Upender Velaparthi, David R. Langley, Xiaopeng Sang, David Frennesson, Joan Carboni, Aixin Li, Ann Greer, Marco Gottardis, Ricardo M. Attar, Zheng Yang, Praveen Balimane, Lorell N. Discenza,