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ASYMMETRIC CATALYTIC REDUCTION OF OXCARBAZEPINE

2025-06-19 02:343720下载
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FIELD : chemistry. SUBSTANCE : described is a method of producing (S)-(+)-10, 11-dihydro-10-hydroxy-5H-dibenz/b, f/azepine-5-carboxamide or R)-(-)-10, 11- dihydro-10-hydroxy-5H-dibenz/b, f/azepine-5-carboxamide by reducing oxcarbazepine in the presence of a catalyst and a hydride source. The catalyst is based on a combination of [RuX2(L)]2, where X is chlorine, bromine or iodine, and L is an acrylic or arylaliphatic ligand, and a ligand of formula or formula , where values of radicals are given in the claim. The hydride source is either NR3R4R5 and formic acid or [R3R4R5NH][OOCH] and, optionally, formic acid, or [M][OOCH)8 and formic acid, where R3, R4 and R5 denote C1-6-alkyl; M denotes an alkali metal or alkali-earth metal and x equals 1 or 2. During the process, pH is kept between 6.5 and 8. The solvent in which reduction takes place contains at least one polar aprotic solvent. EFFECT : efficient method of obtaining the compounds. 30 cl, 4 ex, 5 tbl


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