反应 #433608

ord-43e33272553b40688f8b64afac2e2628

反应方程式

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

反应条件

详细条件
See reaction.notes.procedure_details.

实验过程

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, as described. The 4-[(3-bromophenyl)amino]-6-aminoquinazoline is then reacted with bistributyltin, using tetrakis(triphenylphosphine)palladium in THF solution as the reaction catalyst, as is described hereinbelow. The stanylated quinazoline is then reacted with bromine-76 or bromine-77, in the presence of an oxidizing agent, to produce bromine-76 labeled or bromine-77 labeled 4-[(3-bromophenyl)amino]-6-aminoquinazoline, which is further reacted with 4-bromocrotonyl chloride (obtained by reacting oxalyl chloride and 4-bromocrotonic acid) and dimethylamine, as described, to yield the final bromine-76 labeled or bromine-77 labeled product.

来源

DOI: 10.6084/m9.figshare.5104873.v1专利: US07172749B2uspto-grants-2007_02