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Synthesis of [carbonyl-14C]-labelled remoxipride and raclopride. Two potential neuroleptic agents

✍ Scribed by Lars Gawell

Publisher
John Wiley and Sons
Year
1986
Tongue
French
Weight
209 KB
Volume
23
Category
Article
ISSN
0022-2135

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✦ Synopsis

The synthesis o f two benzamide derivatives labelled with carbon-I4 a t the carboxamide position i s described. The radioactive label was introduced by the reaction o f 1,3-ditnethoxy-2-lithiobenzene w i t h L1'CJcarbon dioxide to furnish 2,6-dimethoxy[~arboxy-~~C]benzoSc acid (2).

followed by reaction w i t h thionyl chloride l e d t o the corresponding labelled acid chlorides. These were reacted with (S)-2-!aminomethyl)-lethylpyrrolidine (5)and converted i n t o [14C]remoxipride (6) and [14C lraclopride (8) -, respectively. Halogenation o f 1 w i t h dioxane dibromide or sulphuryl chloride

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