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author:

Li, Yongjiu (Li, Yongjiu.) [1] | Liu, Xin (Liu, Xin.) [2] | Liu, Qiong (Liu, Qiong.) [3] | Wang, Yuchen (Wang, Yuchen.) [4] | Liu, Chenguang (Liu, Chenguang.) [5] (Scholars:刘晨光) | Chen, Fener (Chen, Fener.) [6]

Indexed by:

EI Scopus SCIE

Abstract:

Aftobetin is a non-invasive diagnosis of Alzheimer ' s disease, that can bind with aggregated beta-amyloid peptide in eye ' s lenses, used for early diagnosis of Alzheimer ' s disease in a rapid and painless mode. The reported synthesis of this probe fell short in the aspects of greenness and economy due to the involvement of toxic Chromium(IV) oxidant, noble palladium catalyst, elevated reaction temperature, the long reaction time as well as the cumbersome workup. Herein, a holistic optimization of the synthetic process was achieved via the employment of flow technology and heterogenous photocatalysis. Firstly, the integration of heterogenous carbon nitrides photocatalysis and circulation flow technology furnished the air oxidation of alcohol and nickel catalyzed C-N coupling at 20 g scale, thus avoiding the use of toxic Chromium and precious palladium species respectively. Flow-intensified esterification between acyl chloride and alcohol, just taking 30 seconds replaced the Steglich esterification of 6 hours, also avoiding the generation of difficult-to-remove dicyclohexylurea. Finally, C-N coupling, esterification and Knoevenagel condensation were telescoped together, thus simplifying the reaction workup. This fully-flow protocol led to the on-demand synthesis of eight probes.

Keyword:

AD probes Aftobetin Flow synthesis technology Heterogenous photocatalysis

Community:

  • [ 1 ] [Li, Yongjiu]Fuzhou Univ, Inst Pharmaceut Sci & Technol, Coll Chem, Fuzhou 350108, Peoples R China
  • [ 2 ] [Liu, Xin]Fuzhou Univ, Inst Pharmaceut Sci & Technol, Coll Chem, Fuzhou 350108, Peoples R China
  • [ 3 ] [Wang, Yuchen]Fuzhou Univ, Inst Pharmaceut Sci & Technol, Coll Chem, Fuzhou 350108, Peoples R China
  • [ 4 ] [Liu, Chenguang]Fuzhou Univ, Inst Pharmaceut Sci & Technol, Coll Chem, Fuzhou 350108, Peoples R China
  • [ 5 ] [Chen, Fener]Fuzhou Univ, Inst Pharmaceut Sci & Technol, Coll Chem, Fuzhou 350108, Peoples R China
  • [ 6 ] [Li, Yongjiu]Qingyuan Innovat Lab, Quanzhou 362801, Peoples R China
  • [ 7 ] [Liu, Xin]Qingyuan Innovat Lab, Quanzhou 362801, Peoples R China
  • [ 8 ] [Liu, Chenguang]Qingyuan Innovat Lab, Quanzhou 362801, Peoples R China
  • [ 9 ] [Chen, Fener]Qingyuan Innovat Lab, Quanzhou 362801, Peoples R China
  • [ 10 ] [Li, Yongjiu]Fuzhou Univ, Fujian Prov Univ, Fujian Prov Univ, Fuzhou 350108, Peoples R China
  • [ 11 ] [Liu, Xin]Fuzhou Univ, Fujian Prov Univ, Fujian Prov Univ, Fuzhou 350108, Peoples R China
  • [ 12 ] [Wang, Yuchen]Fuzhou Univ, Fujian Prov Univ, Fujian Prov Univ, Fuzhou 350108, Peoples R China
  • [ 13 ] [Liu, Chenguang]Fuzhou Univ, Fujian Prov Univ, Fujian Prov Univ, Fuzhou 350108, Peoples R China
  • [ 14 ] [Liu, Qiong]Guangdong Acad Sci, China Natl Analyt Ctr, Inst Anal, Guangdong Prov Key Lab Chem Measurement & Emergenc, Guangzhou 510070, Peoples R China
  • [ 15 ] [Chen, Fener]Fudan Univ, Inst Biomed Sci, Dept Chem, Shanghai 200438, Peoples R China

Reprint 's Address:

  • [Liu, Chenguang]Fuzhou Univ, Inst Pharmaceut Sci & Technol, Coll Chem, Fuzhou 350108, Peoples R China;;[Chen, Fener]Fuzhou Univ, Inst Pharmaceut Sci & Technol, Coll Chem, Fuzhou 350108, Peoples R China;;

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Source :

CHEMSUSCHEM

ISSN: 1864-5631

Year: 2025

Issue: 1

Volume: 18

7 . 5 0 0

JCR@2023

Cited Count:

WoS CC Cited Count:

SCOPUS Cited Count:

ESI Highly Cited Papers on the List: 0 Unfold All

WanFang Cited Count:

Chinese Cited Count:

30 Days PV: 1

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