Iometopane, GPI-200, beta-CIT, RTI-55, Dopascan

(1R,2S,3S,5S)-3-(4-碘苯基)-8-甲基-8-氮杂双环[3.2.1]辛烷-2-羧酸甲酯 (123I)-2beta-甲氧羰基-3beta-(4-碘苯基)莨菪烷 Chemical Name: (-)-1(R)-3-exo-(4-Iodophenyl)-8-methyl-8-azabicyclo[3.2.1]octan-2-exo-yl-carboxylic acid methyl ester; (-)-3beta-(4-Iodophenyl)tropane-2beta-carboxylic acid methyl ester
CAS No. 135416-43-2, 136794-86-0 ([123I]-labeled)
项目整合开发状态: Pre-Registered
项目研究机构: Research Triangle Institute (Originator), Guilford Pharmaceuticals (Licensee), MAP (Licensee), Daiichi Radioisotope (Codevelopment)
合成路线:Treatment of anhydroecgonine methyl ester (I) with phenylmagnesium bromide (II) in Et2O affords a mixture of isomers from which phenyltropane derivative (III) is chromatographically separated.Nitration of (III) using nitronium tetrafluoroborate (NO2BF4) in acetonitrile provides derivative (IV),whose nitro group is then reduced by hydrogenation over Raney-Ni in MeOH to yield the p-amino derivative (V).Finally,the desired product is obtained by treatment of (V) with diiodomethane and isoamyl nitrite (VI).