3-Bromoaniline → N-(3-Bromophenyl)-6-nitroquinazolin-4-amine

Participants

Reaction Steps

3-Bromoaniline is coupled with 4-chloro-6-nitroquinazoline, to produce 4-[(3-bromophenyl)amino]-6-nitroquinazoline, which is reduced thereafter to the corresponding 6-aminoquinazoline. The 4-[(3-bromophenyl)amino]-6-aminoquinazoline is then reacted with bistributyltin, using tetrakis(triphenylphosphine)palladium in triethylamine solution as the reaction catalyst. The stanylated quinazoline is then reacted with iodine-123, iodine-124 or iodine-131, in the presence of an oxidizing agent, to produce iodine-123 labeled, iodine-124 or iodine-131 labeled 4-[(3-bromophenyl)amino]-6-aminoquinazoline, as is described hereinbelow, which is further reacted with acryloyl chloride as described, to yield the final iodine-123 labeled, iodine-124 labeled or iodine-131 labeled product.

Provenance & Evidence