Syntheses of [14C]BAY 59-7939 and its radiolabeled metabolite M-4

被引：3

作者：

Pleiss, U.

Seidel, D.

Grosser, R.

机构：

[1] Bayer HealthCare AG, Drug Metab & Isotope Chem, Global Drug Discovery, D-42096 Wuppertal, Germany

[2] Bayer HealthCare AG, Med Chem, Global Drug Discovery, D-42096 Wuppertal, Germany

来源：

JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS | 2006年 / 49卷 / 11期

关键词：

factor Xa inhibitor; carbon-14; synthesis; amide formation;

D O I：

10.1002/jlcr.1103

中图分类号：

Q5 [生物化学];

学科分类号：

071010 ; 081704 ;

摘要：

BAY 59-7939 is a novel, oral, direct Factor Xa inhibitor in clinical development for the prevention and treatment of thromboembolic diseases. Radiolabeled BAY 597939 was required for drug absorption, distribution, metabolism and excretion (ADME studies). The BAY 59-7939 was labeled with carbon-14 in the carboxamide group in one step in an overall radiochemical yield of 85% starting from 4-{4-[(5S)-5-(aminomethyl)-2-oxo-1,3-oxazolidin-3-yl]phenyl}mor-pholin-3-one and 5-chlorothiophene-2-[C-14]carboxylic acid. The radiolabeled metabolite M-4 was prepared in 77% yield starting from [1-C-14]glycine and 5-chlorothiophene-5-carboxylic acid. Copyright (c) 2006 John Wiley & Sons, Ltd.

引用

页码：929 / 934

页数：6

共 5 条

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[2]

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