MR-18445

合成路线:Phenyl pyrrole (III) was prepared by Clauson-Kaas reaction of 4-methoxy-2-nitroaniline (I) with 2,5-dimethoxytetrahydrofuran (II).Subsequent reduction of the nitro group of (III) using hydrazine and Raney Nickel provided aniline (IV),which was cyclized with phosgene in refluxing toluene to furnish the pyrroloquinoxaline (V).This was chlorinated with POCl3 to obtain the chloroquinoxaline (VI).Finally,nucleophilic substitution in (VI) with N-(4-fluorobenzyl)piperazine (VII) yielded the title compound.

合成路线:A synthesis for the 18F-labeled compound has also been reported.The piperazinylquinoxaline (IX) was obtained from chloroquinoxaline (VI) and excess piperazine (VIII) at 160 C.This was then alkylated with 4-[18F]fluorobenzyl iodide (X) in refluxing CH2Cl2 to provide the labeled product.

参考文献标题:Synthesis of [18F]MR 18445 and its in vivo evaluat
文献作者:Katounina,T.; et al.
参考来源:J Label Compd Radiopharm 1997,40542


合成路线:Phenyl pyrrole (III) was prepared by Clauson-Kaas reaction of 4-methoxy-2-nitroaniline (I) with 2,5-dimethoxytetrahydrofuran (II).Subsequent reduction of the nitro group of (III) using hydrazine and Raney Nickel provided aniline (IV),which was cyclized with phosgene in refluxing toluene to furnish the pyrroloquinoxaline (V).This was chlorinated with POCl3 to obtain the chloroquinoxaline (VI).Finally,nucleophilic substitution in (VI) with N-(4-fluorobenzyl)piperazine (VII) yielded the title compound.

合成路线:A synthesis for the 18F-labeled compound has also been reported.The piperazinylquinoxaline (IX) was obtained from chloroquinoxaline (VI) and excess piperazine (VIII) at 160 C.This was then alkylated with 4-[18F]fluorobenzyl iodide (X) in refluxing CH2Cl2 to provide the labeled product.

参考文献标题:Novel and selective partial agonists of 5-HT3 rece
文献作者:Prunier,H.; Rault,S.; Lancelot,J.-C.; Robba,M.; Renard,P.; Delagrange,P.; Pfeiffer,B.; Caignard,D.H.; Misslin,R.; Guardiola-Lemaitre,B.; Hamon,M.
参考来源:J Med Chem 1997,40(12),1808


合成路线:Phenyl pyrrole (III) was prepared by Clauson-Kaas reaction of 4-methoxy-2-nitroaniline (I) with 2,5-dimethoxytetrahydrofuran (II).Subsequent reduction of the nitro group of (III) using hydrazine and Raney Nickel provided aniline (IV),which was cyclized with phosgene in refluxing toluene to furnish the pyrroloquinoxaline (V).This was chlorinated with POCl3 to obtain the chloroquinoxaline (VI).Finally,nucleophilic substitution in (VI) with N-(4-fluorobenzyl)piperazine (VII) yielded the title compound.

合成路线:A synthesis for the 18F-labeled compound has also been reported.The piperazinylquinoxaline (IX) was obtained from chloroquinoxaline (VI) and excess piperazine (VIII) at 160 C.This was then alkylated with 4-[18F]fluorobenzyl iodide (X) in refluxing CH2Cl2 to provide the labeled product.
参考文献标题:Synthesis and biological investigations of [18F]MR
文献作者:Katounina,T.; Besret,L.; Dhilly,M.; Petit-Taboue,M.C.; Barbelivien,A.; Baron,J.C.; Dauphin,F.; Barre,L.
参考来源:Bioorg Med Chem 1998,6(6),789