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Synthesis of no‐carrier‐added radiobrominated N‐alkylated analogues of spiperone
Author(s) -
Moerlein S. M.,
Laufer P.,
Stöcklin G.
Publication year - 1985
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/jlcr.2580221004
Subject(s) - chemistry , alkylation , spiperone , alkyl , acetic acid , medicinal chemistry , iodide , methyl iodide , bromine , salt (chemistry) , organic chemistry , catalysis , biochemistry , receptor , antagonist
The synthesis of a series of p‐bromo‐3‐N‐alkyl spiperone analogues is described. N‐alkylation was achieved via reaction of the potassium salt of the spiperone lactam ring with alkyl iodide; subsequent reactions with elemental bromine gave the p‐brominated isomers. Optimization studies using no‐carrier‐added (n.c.a.) 77 Br − indicated that radiobromination of N‐alkyl spiperone analogues occurs with higher yields and in shorter reaction times when dichloramine‐T (DCT) is used rather than H 2 O 2 /acetic acid as an oxidant. The production of the title compounds in high effective specific activity with radiochemical yields of 20–30 % using n.c.a. 77 Br − and DCT is reported.