【药物名称】
化学结构式(Chemical Structure):
参考文献No.676780
标题:Synthesis and SAR studies for the inhibition of TNF-alpha production. Part 2. 2-[3-(Cyclopentyloxy)-4-methoxyphenyl]-substituted-1-isoindolinone derivatives
作者:Park, J.S.; Moon, S.C.; Baik, K.U.; Cho, J.Y.; Yoo, E.S.; Byun, Y.S.; Park, M.H.
来源:Arch Pharmacal Res 2002,25(2),137
合成路线图解说明:

Alkylation of 2-methoxy-5-nitrophenol (I) with cyclopentyl bromide (II) provides the cyclopentyl ether (III). Subsequent reduction of the nitro derivative (III) to aniline (IV) is effected by transfer hydrogenation in the presence of ammonium formate and Pd/C. Condensation of 3-(cyclopentyloxy)-4-methoxyaniline (IV) with 4-nitrophthalic anhydride (V) gives rise to phthalimide (VI). Reduction of imide (VI) by means of NaBH4 furnishes the amide alcohol (VII), which is further cyclized to isoindoline (VIII) under Mitsunobu conditions. Finally, transfer hydrogenation of nitro isoindoline (VIII) gives rise to the corresponding amine.

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