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Total synthesis and analgesic activity of 6-fluoroindan-1-acetic acid and its 3-oxo derivative.

机译:6-氟茚满-1-乙酸及其3-氧代衍生物的全合成和止痛活性。

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摘要

6-Fluoro-3-oxo-indan-1-acetic acid (5) and 6-fluoroindan-1-acetic acid (6) were conveniently synthesised from 3-fluorobenzaldehyde in four and five steps, respectively. The structures of these new compounds and two other intermediates, 3-fluorobenzylidine-bis-acetoacetate (2) and 3-fluoro-beta-phenyl glutaric acid (3) were elucidated by spectroscopic means, notably, HRMS, 1D and 2D NMR. The analgesic activity of compounds 5 and 6 were assessed by the acetic acid induced writhing in Swiss albino mice.
机译:由3-氟苯甲醛分别通过四个步骤和五个步骤方便地合成了6-氟-3-氧代-茚满-1-乙酸(5)和6-氟茚满-1-乙酸(6)。通过光谱方法,特别是HRMS,1D和2D NMR阐明了这些新化合物和其他两种中间体的结构,即3-氟苄基双乙酰乙酸酯(2)和3-氟-β-苯基戊二酸(3)。通过乙酸诱导的白化病小鼠扭体来评估化合物5和6的镇痛活性。

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