Synthesis of two non-peptidyl GnRH receptor antagonists via [14C]carbonylation
| Autor: | Dennis C. Dean, Robert J. DeVita, Charles S. Elmore, David G. Melillo |
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| Rok vydání: | 2003 |
| Předmět: |
Bicyclic molecule
Stereochemistry Chemistry medicine.drug_class Organic Chemistry Antagonist Gonadotropin-releasing hormone Metabolism Receptor antagonist Biochemistry Chemical synthesis Analytical Chemistry chemistry.chemical_compound Drug Discovery medicine Lactam Radiology Nuclear Medicine and imaging Carbonylation Spectroscopy |
| Zdroj: | Journal of Labelled Compounds and Radiopharmaceuticals. 46:993-1000 |
| ISSN: | 1099-1344 0362-4803 |
| DOI: | 10.1002/jlcr.733 |
| Popis: | In support of a program to develop a new gonadotropin releasing hormone (GnRH) receptor antagonist, two 14C labelled candidate tracers, 14C-1 and 14C-2, were synthesized for utilization in metabolism studies. A slight modification of the Medicinal Chemistry route for the synthesis of the antagonists provided iodide 4. Palladium (0) catalyzed [14C]carbonylation of 4 proceeded in good chemical yield to afford acid 14C-3 which served as a common precursor to 14C-1 and 14C-2. Copyright © 2003 John Wiley & Sons, Ltd. |
| Databáze: | OpenAIRE |
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