## Abstract The preparation of [^3^H]Sch 727965 from unlabeled compound and tritiated water was base catalyzed. Diethyl [^13^C~3~]malonate was used to prepare [^13^C~3~]Sch 727965 in five steps in 21.8% overall yield. In a similar manner, [^14^C]Sch 727965 was prepared in five steps from diethyl [2
Synthesis of [3H], [13C215N] and [14C]Sch 66336 (Sarasar™)
✍ Scribed by D. Hesk; D. Cesarz; C. Magatti; K. Voronin; C. Lavey; P. McNamara; D. Koharski; S. Saluja; S. Hendershot; H. Pham; V. Truong
- Publisher
- John Wiley and Sons
- Year
- 2005
- Tongue
- French
- Weight
- 141 KB
- Volume
- 48
- Category
- Article
- ISSN
- 0022-2135
- DOI
- 10.1002/jlcr.891
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✦ Synopsis
Abstract
[^3^H]Sch 66336 was prepared at a specific activity of 1.35 Ci/mmol by Ru(Ph~3~P)~3~Cl~2~ catalysed exchange with tritiated water. [^13^CN]Sch 66336 was synthesized from potassium [^13^C]cyanide and [^13^C^15^N~2~]urea in 29% overall yield from potassium [^13^C]cyanide. [^14^C]Sch 66336 was synthesized from potassium [^14^C]cyanide in 31% yield. A second synthesis, from N‐Boc‐4‐hydroxy[^14^C]piperidine, gave [^14^C]Sch 66336 labelled in a different site in 19% overall yield. Copyright © 2004 John Wiley & Sons, Ltd.
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