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Improved synthesis of anxiolytic, anticonvulsant, and antinociceptive α2/α3-GABA(A)-ergic receptor subtype selective ligands as promising agents to treat anxiety, epilepsy, and neuropathic pain
Li, G., Golani, L., Jahan, R., Rashid, F., & Cook, J. (2018). Improved synthesis of anxiolytic, anticonvulsant, and antinociceptive α2/α3-GABA(A)-ergic receptor subtype selective ligands as promising agents to treat anxiety, epilepsy, and neuropathic pain. Synthesis, 50(20), 4124-4132. https://doi.org/10.1055/s-0037-1610211
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.