The synthesis of a tritium, carbon-14, and stable isotope-labeled cathepsin C inhibitors.
J Labelled Comp Radiopharm
; 60(2): 124-129, 2017 02.
Article
in En
| MEDLINE
| ID: mdl-27868229
ABSTRACT
As part of a medicinal chemistry program aimed at developing a highly potent and selective cathepsin C inhibitor, tritium, carbon-14, and stable isotope-labeled materials were required. The synthesis of tritium-labeled methanesulfonate 5 was achieved via catalytic tritiolysis of a chloro precursor, albeit at a low radiochemical purity of 67%. Tritium-labeled AZD5248 was prepared via a 3-stage synthesis, utilizing amide-directed hydrogen isotope exchange. Carbon-14 and stable isotope-labeled AZD5248 were successfully prepared through modifications of the medicinal chemistry synthetic route, enabling the use of available labeled intermediates.
Key words
Full text:
1
Collection:
01-internacional
Database:
MEDLINE
Main subject:
Tritium
/
Biphenyl Compounds
/
Cysteine Proteinase Inhibitors
/
Radiopharmaceuticals
/
Cathepsin C
Language:
En
Journal:
J Labelled Comp Radiopharm
Year:
2017
Document type:
Article
Affiliation country:
United kingdom