期刊
MOLECULES
卷 27, 期 21, 页码 -出版社
MDPI
DOI: 10.3390/molecules27217594
关键词
dimethindene; deep eutectic solvents; API synthesis; synthetic methodologies; green chemistry; cyclopentyl methyl ether; 2-Methyltetrahydrofuran
资金
- FSE-FESR [1377]
- Ministero dell'Universita e della Ricerca (MUR) through the PRIN project Unlocking Sustainable Technologies Through Nature-Inspired Solvents (NATUREChem) [2017A5HXFC_002]
- MCIN/AEI [CTQ2016-75986-P, RED2018-102387-T, PID2020-113473GB-I00]
The use of eco-friendly solvents 2-MeTHF and CPME in the synthesis of dimethindene was found to reduce environmental impact, increase synthesis yield, and simplify manual operations.
Dimethindene is a selective histamine H-1 antagonist and is commercially available as a racemate. Upon analyzing the synthetic pathways currently available for the industrial preparation of dimethindene, we set up a sustainable approach for the synthesis of this drug, switching from petroleum-based volatile organic compounds (VOCs) to eco-friendly solvents, such as 2-methyltetrahydrofuran (2-MeTHF) and cyclopentyl methyl ether (CPME) belonging to classes 3 and 2, respectively. Beyond decreasing the environmental impact of the synthesis (E-factor: 24.1-54.9 with VOCs; 12.2-22.1 with 2-MeTHF or CPME), this switch also improved the overall yield of the process (from 10% with VOCs to 21-22% with 2-MeTHF or CPME) and remarkably simplified the manual operations, working under milder conditions. Typical metrics applied at the first and second pass, according to the CHEM21 metrics toolkit, were also calculated for the whole synthetic procedure of dimethindene, and the results were compared with those of the classical procedure.
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