A facile and efficient method for the synthesis of crystalline tetrahydro-β-carbolines via the Pictet-Spengler reaction in water

被引：8
|
作者：
Byeon, Hong-Ju [1 ]
Jung, Kyung-Hwan [1 ]
Moon, Gi-Seong [1 ]
Moon, Sung-Kwon [2 ]
Lee, Hyang-Yeol [1 ]
机构：
[1] Korea Natl Univ Transportat, Dept Biotechnol, 61 Daehak Ro, Chungbuk 27909, South Korea
[2] Chung Ang Univ, Dept Food & Nutr, 4726 Seodong Daero, Anseong 456756, South Korea
来源：
SCIENTIFIC REPORTS | 2020年 / 10卷 / 01期
基金：
新加坡国家研究基金会;
关键词：
CATALYSIS;
D O I：
10.1038/s41598-020-57911-0
中图分类号：
O [数理科学和化学]; P [天文学、地球科学]; Q [生物科学]; N [自然科学总论];
学科分类号：
07 ; 0710 ; 09 ;
摘要：
A facile and efficient synthesis of tetrahydro-beta-carbolines (tryptolines) in one step from tryptamine and aldehydes, in an environmentally friendly water solvent, has been investigated. This convenient and clean synthesis of various tryptolines was facilitated by l-tartaric acid, a natural compound, to obtain the desired products as clear crystals. Among the four crystalline products, the most substituted tryptoline 2 showed the best inhibitory activity against EJ cells and the least cytotoxicity, with an LC50 value of 1.49 mg/mL, against brine shrimp larvae.
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页数：6
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