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吲哚克酮酸的合成及其作为光声成像造影剂的初步研究
引用本文:鲁亮,郭丽,胡曰富,齐庆蓉.吲哚克酮酸的合成及其作为光声成像造影剂的初步研究[J].合成化学,2017,25(4):287-290.
作者姓名:鲁亮  郭丽  胡曰富  齐庆蓉
作者单位:四川大学 华西药学院,四川 成都 610041
基金项目:重大新药创制:石药集团心脑血管药物创新综合平台建设
摘    要:以克酮酸和2,3,3-三甲基-3H-吲哚为原料,经缩合反应合成了吲哚克酮酸(ICR),其结构经1H NMR和MS确证。并将ICR作为光声成像造影剂进行了初步研究。结果表明:ICR在近红外区的吸收强烈且尖锐,最大吸收波长为755 nm,发射波长为775 nm,摩尔吸光系数为4.14×105 L·mol-1·cm-1; ICR的体外光声成像造影效果远大于吲哚菁绿(ICG),在浓度为21.6 μmol·L-1时,ICR的光声强度是ICG的52万倍。

关 键 词:克酮酸  2  3  3-三甲基-3H-吲哚  吲哚克酮酸  合成  光声成像  近红外区  吲哚菁绿  
收稿时间:2016-12-13

Synthesis and Preliminary Study of IndoleCroconium as Photoacoustic Imaging Contrast Agent
LU Liang,GUO Li,HU Yue-fu,QI Qing-rong.Synthesis and Preliminary Study of IndoleCroconium as Photoacoustic Imaging Contrast Agent[J].Chinese Journal of Synthetic Chemistry,2017,25(4):287-290.
Authors:LU Liang  GUO Li  HU Yue-fu  QI Qing-rong
Abstract:Indole croconium(ICR) was synthesized by condensation reaction of croconic acid with 2,3,3-trimethylindolenine.The structure was confirmed by 1H NMR and MS.The preliminary study of ICR as a photoacoustic imaging contrast agent was investigated.The results showed that ICR exhibited a sharp and strong absorption in the near infrared region, the maximum absorption wavelength was 755 nm and emission wavelength was 775 nm, and the molar absorption coefficient was 4.14×105 L·mol-1·cm-1.The photoacoustic imaging effect of ICR was far better than that of the indocyanine green(ICG).Photoacoustic intensity of ICR was 520 000 times of that of ICG at the concentration of 21.6 μmol·L-1.
Keywords:croconic acid  2  3  3-trimethylindolenine  indole croconium  synthesis  photoacoustic imaging  near infrared region  indocyanine green
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