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Novel Synthesis of 4-Benzylidene-2-((1-phenyl-3,4-dihydroisoquinoline-2(1H)-yl)methyl) oxazol-5(4H)-one Derivatives Using 1,2,3,Tetrahydroisoquinoline and their Antimicrobial Activity.
Current Organic Synthesis ( IF 1.7 ) Pub Date : 2020-07-31 , DOI: 10.2174/1570179417666200415151228
Nalla Krishna Rao 1 , Tentu Nageswara Rao 2 , Botsa Parvatamma 3 , Y Prashanthi 4 , Ravi Kumar Cheedarala 5
Affiliation  

Aims: A series of six 4-benzylidene-2-((1-phenyl-3,4-dihydro isoquinoline-2(1H)-yl)methyloxazol- 5(4H)-one derivatives were synthesized by condensation of substituted aryl aldehydes with 2-(2-(1-phenyl-3,4- dihydro isoquinoline-2(1H)-acetamido)acetic acid in the presence of sodium acetate, acetic anhydride and zinc oxide as catalysts.

Background: Novel Synthesis of 4-Benzylidene-2-((1-phenyl-3,4-dihy droisoquinoline-2(1H)-yl)methyl)oxazol- 5(4H)-one derivatives using 1,2,3,Tetrahydroisoquinoline and their antimicrobial activity.

Objective: The title compounds can be synthesized from 1,2,3,4-tetrahydroisoquinoline.

Methods: The target molecules, i.e., 4-benzylidene-2-((1-phenyl-3, 4-dihydro isoquinoline-2(1H)-yl) methyl) oxazol-5(4H)-one derivatives (8a-8f) have been synthesized from 1,2,3,4-tetrahydroisoquinoline which was prepared from benzoic acid in few steps.

Results: All the six compounds were evaluated based on advanced spectral data (1H NMR, 13C NMR & LCMS), and the chemical structures of all compounds were determined by elemental analysis.

Conclusion: Antibacterial activity of the derivatives was examined for the synthesized compounds and results indicate that compound with bromine substitution has a good activity profile.



中文翻译:

使用1,2,3,四氢异喹啉及其抗菌剂新型合成4-苄叉-2-((1-苯基-3,4-二氢异喹啉-2(1H)-基)甲基)恶唑-5(4H)-one衍生物活动。

目的:通过取代的芳基醛缩合,合成了一系列的六个4-亚苄基-2-(((1-苯基-3,4-二氢异喹啉-2(1H)-基)甲基恶唑-5(4H)-一)衍生物在乙酸钠,乙酸酐和氧化锌作为催化剂存在下的2-(2-(1-苯基-3,4-二氢异喹啉-2(1H)-乙酰氨基)乙酸。

背景:使用1,2,3,四氢异喹啉新颖合成4-苄叉基-2-((1-苯基-3,4-二氢droisoquinoline-2(1H)-基)甲基)恶唑-5(4H)-一衍生物及其抗菌活性。

目的:可由1,2,3,4-四氢异喹啉合成标题化合物。

方法:目标分子,即4-亚苄基-2-(((1-苯基-3,4-二氢异喹啉-2(1H)-基)甲基)恶唑-5(4H)-一衍生物(8a-8f)已经由1,2,3,4-四氢异喹啉合成,它是由苯甲酸在几个步骤中制备的。

结果:根据先进的光谱数据(1H NMR,13C NMR和LCMS)对所有6种化合物进行了评估,并通过元素分析确定了所有化合物的化学结构。

结论:检测了该衍生物对合成化合物的抗菌活性,结果表明具有溴取代基的化合物具有良好的活性。

更新日期:2020-07-31
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