B. Vu, Dinh Chau Phan, Thi Hong Long Nguyen
Jan 23, 2023
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Letters in Organic Chemistry
Abstract
Synthesis Memantine and Memantine Hydrochloride by Direct Amination of 1-Bromo-3,5-dimethyladamantane with thiourea, optimizing the reaction parameters Memantine hydrochloride (MH) is a first-line therapeutic drug approved by the US FDA for the management of moderate to severe Alzheimer's disease To optimize the synthesis process of memantine hydrochloride by direct aminoation of 1-bromo-3,5-dimethyladamantane with thiourea Using the basic chemical reactions to optimize the reaction conditions The optimal conditions of the memantine hydrochloride process include: the reaction temperature was 160oC in first step and 800C in second step; the total time reaction was 5.5 hrs; the molar ratio of 2: thiourea: PG: HCl was 1:4: 8: 8; overall yields 83.11%. The obtained product have been determined by IR, MS and H-NMR spectra and high pure (GC 99.91%). the process for synthesizing memantine hydrochloride from 1-bromo-3,5-dimethyladamantane and thiourea has been established, which is simpler, safer and more econominal. ACKNOWLEDGMENT This research was financially supported by Drug R&D Center, VMMU, Vietnam.