Synthesis of a delta opioid agonist in [2H6], [2H4], [11C], and [14C] labeled forms

被引：9

作者：

Elmore, Charles S. ^{[1
]}

Brush, Kelly ^{[2
]}

Schou, Magnus ^{[4
,5
]}

Palmer, William ^{[2
]}

Dorff, Peter N. ^{[2
]}

Powell, Mark E. ^{[2
]}

Hoesch, Valerie ^{[2
]}

Hall, James E. ^{[2
]}

Hudzik, Thomas ^{[3
]}

Halldin, Christer ^{[5
]}

Dantzman, Cathy L. ^{[2
]}

机构：

[1] AstraZeneca Pharmaceut LP, Isotope Chem, DMPK, Wilmington, DE 19850 USA

[2] AstraZeneca Pharmaceut LP, CNS Chem, Wilmington, DE 19850 USA

[3] AstraZeneca Pharmaceut LP, Neurosci Biol, Wilmington, DE 19850 USA

[4] AstraZeneca, CNS Chem, SE-15185 Sodertalje, Sweden

[5] Karolinska Univ Hosp, Karolinska Inst, Dept Clin Neurosci, Psychiat Sect, SE-17176 Stockholm, Sweden

来源：

JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS | 2011年 / 54卷 / 14期

关键词：

2H6]quinolin-8-ol; 2H4]ethanolamine; 14C]carbonylation; 11C]methylation; RAT;

D O I：

10.1002/jlcr.1939

中图分类号：

Q5 [生物化学];

学科分类号：

071010 ; 081704 ;

摘要：

In support of a program to develop a treatment for depression, four labeled forms of a delta opioid agonist were prepared. The [2H4] labeled form was prepared using a relatively straightforward conversion of [2H4]bromoethanol to [2H4]N-methyl-2-hydroxyethylamine. The key step in the synthesis of the [2H6] labeled form involved the Pd-catalyzed exchange in D2O of 8-quinolin-8-ol to give [2H6] 8-quinolin-8-ol. The C-14 labeled form was synthesized in one step using [14C]carbonylation, and the C-11 labeled form was prepared in two steps from 11CH3I. Copyright (C) 2011 John Wiley & Sons, Ltd.

引用

页码：847 / 854

页数：8

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