Radiolabeled 4-phenylquinazoline-2-carboxamides of general formula I (wherein X is O or S, R1 is H or Cl, R2 is C1-C6 alkyl, R3 is 11CH3, R4 is H or Cl, and R is H; X is O or S, R1 is F, R2 is C1-C6 alkyl, R3 is 11CH3, R4 is H, and R is H or NO2; or X is O or S, R1 is 18F, R2 is C1-C6 alkyl, R3 is CH3, R4 is H, and R is H or NO2) useful as imaging agents for positron emission tomog. of translocator protein (TSPO) are described. Methods of detecting TSPO and neuroinflammation using the compds. are described. Also disclosed are radiolabeling methods for selected compds. Example compd. II was prepd. by reacting 4-(2-fluorophenyl)quinazoline-2-carboxylic acid and (R)-butan-2-amine and reacting the intermediate formed with a 11C-methylating agent. II was examd. as a radioligand in various bioassays
Preparation of radiolabeled 4-phenylquinazoline-2-carboxamides for detecting translocator protein and neuroinflammation diagnosis
DA SETTIMO PASSETTI, FEDERICO;MARTINI, CLAUDIA;TALIANI, SABRINA;
2014-01-01
Abstract
Radiolabeled 4-phenylquinazoline-2-carboxamides of general formula I (wherein X is O or S, R1 is H or Cl, R2 is C1-C6 alkyl, R3 is 11CH3, R4 is H or Cl, and R is H; X is O or S, R1 is F, R2 is C1-C6 alkyl, R3 is 11CH3, R4 is H, and R is H or NO2; or X is O or S, R1 is 18F, R2 is C1-C6 alkyl, R3 is CH3, R4 is H, and R is H or NO2) useful as imaging agents for positron emission tomog. of translocator protein (TSPO) are described. Methods of detecting TSPO and neuroinflammation using the compds. are described. Also disclosed are radiolabeling methods for selected compds. Example compd. II was prepd. by reacting 4-(2-fluorophenyl)quinazoline-2-carboxylic acid and (R)-butan-2-amine and reacting the intermediate formed with a 11C-methylating agent. II was examd. as a radioligand in various bioassaysI documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
