【药物名称】PE2Br
化学结构式(Chemical Structure):
参考文献No.300222
标题:Synthesis, ligand binding, QSAR, and CoMFA study of 3beta-(p-substitutedphenyl)tropane-2beta-carboxylic acid methyl esters
作者:Gao, Y.; Rahman, M.A.; Abraham, P.; Boja, J.W.; Carroll, F.I.; Lewin, A.H.; Kuhar, M.J.; Parham, K.
来源:J Med Chem 1991,34(9),2719
合成路线图解说明:

The reaction of anhydroecgonine methyl ester (I) with 4-methylphenylmagnesium bromide (II) in ethyl ether gives 3beta-(4-methylphenyl)tropane-2beta-carboxylic acid methyl ester (III), which is demethylated by reaction with 2,2,2-trichloroethyl chloroformate (IV) yielding the carbamate (V), followed by reduction with Zn/AcOH to afford the nortropane derivative (VI). The alkylation of (VI) with the tributylstannane (VII), TEA and iodine in ethanol provides the adduct (VIII), which is finally brominated with NBS in THF.

参考文献No.541598
标题:Synthesis of (E)-N-(3-bromoprop-2-enyl)-2 beta-carbomethoxy-3 beta-(4 '-tolyl) nortropane (PE2Br) and radiolabelling of [Br-76]PE2Br: A potential ligand for exploration of the dopamine transporter by PET
作者:Helfenbein, J.; et al.
来源:J Label Compd Radiopharm 1999,42(6),581
合成路线图解说明:

The reaction of anhydroecgonine methyl ester (I) with 4-methylphenylmagnesium bromide (II) in ethyl ether gives 3beta-(4-methylphenyl)tropane-2beta-carboxylic acid methyl ester (III), which is demethylated by reaction with 2,2,2-trichloroethyl chloroformate (IV) yielding the carbamate (V), followed by reduction with Zn/AcOH to afford the nortropane derivative (VI). The alkylation of (VI) with the tributylstannane (VII), TEA and iodine in ethanol provides the adduct (VIII), which is finally brominated with NBS in THF.

参考文献No.607780
标题:Compounds affecting the central nervous system. 4. 3beta-Phenyltropane-2-carboxylic esters and analogs
作者:Clarke, R.L.; Daum, S.J.; Gambino, A.J.; Aceto, M.D.; Pearl, J.; Levitt, M.; Cumiskey, W.R.; Bogado, E.F.
来源:J Med Chem 1973,16(1),1260-67
合成路线图解说明:

By condensation of (-)-anhydroecgonine methyl ester (I) with 4-fluorophenylmagnesium bromide (II) by means of cuprous chloride in refluxing ether.

合成路线图解说明:

The reaction of anhydroecgonine methyl ester (I) with 4-methylphenylmagnesium bromide (II) in ethyl ether gives 3beta-(4-methylphenyl)tropane-2beta-carboxylic acid methyl ester (III), which is demethylated by reaction with 2,2,2-trichloroethyl chloroformate (IV) yielding the carbamate (V), followed by reduction with Zn/AcOH to afford the nortropane derivative (VI). The alkylation of (VI) with the tributylstannane (VII), TEA and iodine in ethanol provides the adduct (VIII), which is finally brominated with NBS in THF.

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