Abstract
Propranolol is one of the first medications of the beta-blocker used for antihypertensive drugs. This study reports the facile route for the synthesis of propranolol and its novel derivatives. Herein, propranolol synthesis proceeded from 1-naphthol and isopropylamine under mild and less toxic conditions. Novel propranolol derivatives were designed by reactions of propranolol with benzoyl chloride, pyridinium chlorochromate, and n-butyl bromide through esterification, oxidation reduction, and alkylation, respectively. The isolation and purity of compounds were conducted using column chromatography and thin-layer chromatography. Mass spectrometry and 1H-NMR spectroscopy were applied to identify new compounds structure. Propranolol derivatives from 2-chlorobenzoyl chloride (compound 3), 2-fluorobenzoyl chloride (compound 5), and especially acetic anhydride (compound 6) manifested high yields and significantly increased water solubility. Six semisynthetic propranolol derivatives promise to improve antioxidative and biological activities.
Highlights
Propranolol is one of the original medicines of the betablocker used to treat hypertension, tremors, angina, and cardiovascular disorders [1, 2]
Silica gel 230–400 mesh for column chromatography was purchased from HiMedia (India)
2.2.1. in-Layer Chromatography (TLC). 5 μL of sample and standard solutions was dropped on a TLC plate, which was immersed in ethyl acetate : hexane system at different ratios. e moving of the mobile phase was finished until it reached the highest limitation of the TLC plate. e separated TLC plate was dried at room temperature (RT) for 30 min and observed under visible light or UV light
Summary
Propranolol is one of the original medicines of the betablocker used to treat hypertension, tremors, angina, and cardiovascular disorders [1, 2]. Propranolol is an effective and safe drug for treating migraine headaches, anxiety disorders, and infantile hemangiomas [3, 4]. Several studies have recently reported that patients receiving propranolol reduced the risk of neck and head, colon, stomach, and prostate cancers [5,6,7]
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