Synthesis of [3H], [13C215N] and [14C]Sch 66336 (Sarasar™)

Hesk, D., Cesarz, D., Magatti, C., Voronin, K., Lavey, C., Mcnamara, P., Koharski, D., Saluja, S., Hendershot, S., Pham, H., & Truong, V. (2005). Synthesis of [3H], [13C215N] and [14C]Sch 66336 (Sarasar™). Journal of Labelled Compounds and Radiopharmaceuticals, 48(1), 11-23. https://doi.org/10.1002/jlcr.v48:1

Abstract

[3H]Sch 66336 was prepared at a specific activity of 1.35 Ci/mmol by Ru(Ph3P)3Cl2 catalysed exchange with tritiated water. [13Curn:x-wiley:03624803:media:JLCR891:tex2gif-stack-1N]Sch 66336 was synthesized from potassium [13C]cyanide and [13C15N2]urea in 29% overall yield from potassium [13C]cyanide. [14C]Sch 66336 was synthesized from potassium [14C]cyanide in 31% yield. A second synthesis, from N‐Boc‐4‐hydroxy[14C]piperidine, gave [14C]Sch 66336 labelled in a different site in 19% overall yield. Copyright © 2004 John Wiley & Sons, Ltd.

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