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Synthesis of a carbon-14 labeled 1-(indole-6-carbonyl-D-phenylglycinyl)-4-(1-methylpiperidin-4-YL)piperazine-[carbonyl-14C], LY517717-[14C], a factor Xa inhibitor

✍ Scribed by Fengjiun Kuo; Dean K. Clodfelter; Tamara R. Priest; Donald L. K. Kau

Publisher
John Wiley and Sons
Year
2004
Tongue
French
Weight
118 KB
Volume
47
Category
Article
ISSN
0022-2135

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✦ Synopsis

Abstract

Human Factor Xa is a trypsin‐like serine protease, which serves a critical role in blood coagulation events. LY517717 is currently under clinical investigation as a Factor Xa inhibitor. To support the ADME studies, LY517717 was synthesized using D‐phenylglycine with a carbon‐14 labeled carboxyl moiety. This key component, D‐phenylglycine‐[carboxyl‐^14^C], was synthesized by a Strecker synthesis on benzaldehyde with potassium [^14^C]cyanide, followed by a resolution of DL‐phenyl‐glycine methyl ester‐[carbonyl‐^14^C] with (+)‐tartaric acid in the presence of benzaldehyde. Copyright © 2004 John Wiley & Sons, Ltd.

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