A Method for Parallel Solid-Phase Synthesis of Iodinated Analogues of the CB1 Receptor Inverse Agonist Rimonabant
| Autor: | George J. Ellames, Teyrnon C. Jones, Andrew D. Kohler, Chih-Chung Tseng, Alan C. Spivey |
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| Jazyk: | angličtina |
| Rok vydání: | 2009 |
| Předmět: |
Cannabinoid receptor
Drug Inverse Agonism Halogenation Stereochemistry Chemistry medicine.medical_treatment Organic Chemistry Biochemistry Structure-Activity Relationship Solid-phase synthesis Piperidines Receptor Cannabinoid CB1 Rimonabant medicine Pyrazoles Inverse agonist lipids (amino acids peptides and proteins) Cannabinoid Physical and Theoretical Chemistry Receptor medicine.drug |
| Popis: | A method for the parallel solid-phase synthesis (SPS) of iodinated analogues of Sanofi-Aventis' type 1 cannabinoid (CB1) receptor inverse agonist rimonabant (acomplia) has been developed. The method allows the synthesis of a range of C3 amide/hydrazide derivatives from a resin-bound C3 ester precursor. The C-Ge linkage to the Hypogel-200 resin is stable to the diversification conditions but allows ipso-iododegermylative cleavage using NaI/NCS even for the products containing the oxidatively labile hydrazide moiety. |
| Databáze: | OpenAIRE |
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