Synthesis of supposed enone prodrugs of apomorphine and N-propyl-norapomorphine
| Autor: | Danyang Liu, Bastiaan J. Venhuis, Durk Dijkstra, Hakan Wikstrom |
|---|---|
| Přispěvatelé: | Molecular Biophysics, Medicinal Chemistry, Groningen Research Institute of Pharmacy |
| Rok vydání: | 2007 |
| Předmět: |
Agonist
medicine.drug_class Stereochemistry retro-synthetic apomorphine Biochemistry chemistry.chemical_compound PARKINSONS-DISEASE In vivo Drug Discovery medicine ring opening DOPAMINERGIC PRODRUG AGENTS PHARMACOLOGY ANALOGS Chemistry Organic Chemistry Dopaminergic ESTERS Propyl-norapomorphine enone-prodrug Prodrug Apomorphine Catecholamine Enone medicine.drug |
| Zdroj: | Tetrahedron, 63(30), 7264-7270. PERGAMON-ELSEVIER SCIENCE LTD |
| ISSN: | 0040-4020 |
| DOI: | 10.1016/j.tet.2007.04.103 |
| Popis: | We have previously demonstrated that the enone prodrug GMC-6650 acts as a highly efficient dopaminergic agonist. In vivo, this compound is bioactivated to its corresponding catecholamine, TL-334. The goal here was to investigate if this bioactivation also occurs for the supposed enone prodrug of apomorphine. We describe the 12-step synthesis of this supposed prodrug, 6-alkyl-5,6,6a,8,9,10-hexahydro-4H-dibenzo[de,g]quinolin-11(7H)-one (R=Me, n-Pr). (C) 2007 Elsevier Ltd. All rights reserved. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
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