Synthesis of 3,4‐dihydro‐5‐[ 11 C]methoxy‐1(2H)‐isoquinolinone as a potential tracer for poly(ADP‐ribose) synthetase | Zendy

Miyake Yoshinori | Zendy; Shimadzu Hiroshi | Zendy; Hashimoto Naoto | Zendy; Ishida Yoshio | Zendy; Shibakawa Masahiko | Zendy; Nishimura Tsunehiko | Zendy

AI Assistant Blog Pricing

Home ZAIA Blog

Premium

Synthesis of 3,4‐dihydro‐5‐[ 11 C]methoxy‐1(2H)‐isoquinolinone as a potential tracer for poly(ADP‐ribose) synthetase

Author(s) -

Miyake Yoshinori,

Shimadzu Hiroshi,

Hashimoto Naoto,

Ishida Yoshio,

Shibakawa Masahiko,

Nishimura Tsunehiko

Publication year - 2000

Publication title -

journal of labelled compounds and radiopharmaceuticals

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 0.432

H-Index - 47

eISSN - 1099-1344

pISSN - 0362-4803

DOI - 10.1002/1099-1344(200009)43:10<983::aid-jlcr383>3.0.co;2-c

Subject(s) - chemistry , sodium azide , yield (engineering) , trifluoromethanesulfonate , specific activity , stereochemistry , radiochemistry , organic chemistry , enzyme , catalysis , materials science , metallurgy

Synthesis of 3,4‐dihydro‐5‐[ 11 C]methoxy‐1(2H)‐isoquinolinone ([ 11 C]MIQO), a potent poly (ADP‐ribose) synthetase inhibitor, was devised in order to evaluate whether it is possible to image excessive activation of poly (ADP‐ribose) synthetase (PARS) by positron emission tomography. [ 11 C]MIQO was prepared by O‐[ 11 C]methylation of 3,4‐dihydro‐5‐hydroxy‐1(2H)‐isoquinolinone, obtained by a Schmidt reaction with 4‐hydroxy‐1‐indanone, sodium azide and trichloroacetic acid, with [ 11 C]methyl triflate. Total synthesis time from EOB was 35 minutes. The radiochemical yield based on [ 11 C]carbon dioxide was 31±8% (n=8; decay corrected). The final product had a specific activity of 76 GBq/μmol at EOS, and the radiochemical purity of [ 11 C]MIQO was over 99%. Copyright © 2000 John Wiley & Sons, Ltd.

This content is not available in your region!

Continue researching here.

Having issues? You can contact us here

Accelerating Research