Development of a Manufacturing Process for 1-(1-Pyridin-2-yl methyl-piperidin-4-yl)-1 H-indole: A Key Intermediate for Protein Kinase C Inhibitor LY317615

S Boini, KP Moder, RK Vaid, M Kopach…

Index: Boini, Sathish; Moder, Kenneth P.; Vaid, Radhe K.; Kopach, Micheal; Kobierski Organic Process Research and Development, 2006 , vol. 10, # 6 p. 1205 - 1211

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Citation Number: 6

Abstract

This contribution describes process development leading to the production of 1-(1-pyridin-2- yl methyl-piperidin-4-yl)-1 H-indole (11). The title compound 11 was produced via a Leimgruber-Batcho indole synthesis using key intermediates 2-(2, 2-dimethoxyethyl) benzenamine (6) and, 1-(2-pyridinylmethyl)-4-piperidinone camphor sulfonate (9). Direct crystallization of 11 from IPA or ethanol-water was developed to provide (11) with< 1% ...

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