تفاعل #433612

ord-c1cc0f27f7a647b6b8cf7f700c7d1a83

معادلة التفاعل

Nc1cccc(Br)c1
3-Bromoaniline
O=[N+]([O-])c1ccc2ncnc(Cl)c2c1
4-chloro-6-nitroquinazoline
O=[N+]([O-])c1ccc2ncnc(Nc3cccc(Br)c3)c2c1
4-[(3-bromophenyl)amino]-6-nitroquinazoline

الكواشف

لا شيء

ظروف التفاعل

الظروف التفصيلية
See reaction.notes.procedure_details.

الإجراء التجريبي

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, as is described hereinabove. The stanylated quinoline is then reacted with iodine-123 or iodine-131, in the presence of an oxidizing agent, to produce iodine-123 labeled or iodine-131 labeled 4-[(3-iodophenyl)amino]-6-aminoquinazolie, which is further reacted with 4-bromocrotonyl chloride and dimethylaniline, as described, to yield the final iodine-123 or iodine-131 labeled product.

المصدر

DOI: 10.6084/m9.figshare.5104873.v1براءة الاختراع: US07172749B2uspto-grants-2007_02