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Facile Synthesis of Propranolol and Novel Derivatives
Journal of Chemistry ( IF 2.8 ) Pub Date : 2020-08-24 , DOI: 10.1155/2020/9597426
Vy Anh Tran 1, 2 , Nguyen Hai Tai Tran 3 , Long Giang Bach 4 , Trinh Duy Nguyen 5 , Thi Thuong Nguyen 5 , Tan Tai Nguyen 6 , Thi Anh Nga Nguyen 7 , The Ky Vo 8 , Thu-Thao Thi Vo 2 , Van Thuan Le 2, 9
Affiliation  

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.

中文翻译:

普萘洛尔及其新型衍生物的简便合成

心得安是用于抗高血压药物的β受体阻滞剂的首批药物之一。本研究报告了合成普萘洛尔及其新型衍生物的简便途径。在此,普萘洛尔在温和且毒性较小的条件下由 1-萘酚和异丙胺合成。通过将普萘洛尔与苯甲酰氯、氯铬酸吡啶鎓和正丁基溴分别通过酯化、氧化还原和烷基化反应设计了新型普萘洛尔衍生物。使用柱色谱和薄层色谱进行化合物的分离和纯度。质谱和 1H-NMR 光谱用于鉴定新的化合物结构。来自 2-氯苯甲酰氯(化合物 3)、2-氟苯甲酰氯(化合物 5)的心得安衍生物,尤其是乙酸酐(化合物 6)表现出高产率和显着增加的水溶性。六种半合成的心得安衍生物有望提高抗氧化和生物活性。
更新日期:2020-08-24
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