Improved Synthesis of Anxiolytic, Anticonvulsant and Antinociceptive α2/α3-GABA(A)ergic Receptor Subtype Selective Ligands as Promising Agents to Treat Anxiety, Epilepsy, as well as Neuropathic Pain
| Autor: | James M. Cook, Rajwana Jahan, Farjana Rashid, Guanguan Li, Lalit K. Golani |
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| Rok vydání: | 2020 |
| Předmět: |
0301 basic medicine
GABAA receptor Chemistry medicine.drug_class medicine.medical_treatment Organic Chemistry Imine Pharmacology Anxiolytic Catalysis Article 03 medical and health sciences chemistry.chemical_compound 030104 developmental biology 0302 clinical medicine Column chromatography Anticonvulsant Reagent Neuropathic pain medicine Selective reduction 030217 neurology & neurosurgery |
| Zdroj: | Synthesis (Stuttg) |
| ISSN: | 0039-7881 |
| Popis: | An improved synthesis of the anxiolytic, anticonvulsant, and antinociceptive compounds: Hz-166, and its bioisosteres 1,2,4-oxadiazole (MP-III-080) and 1,3-oxazole (KRM-II-81) were synthesized in higher yields and with more facile purification methods (crystallization, etc.) in multigram quantities without column chromatography. In the synthesis of KRM-II-81, an alternative procedure was employed using the selective reducing reagent, potassium diisobutyl-tert-butoxyaluminum hydride (PDBBA), to prepare the desired C(3)-aldehyde in the absence of N(5)–C(6) imine reduction in good yield on a 20 gram scale. |
| Databáze: | OpenAIRE |
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