新产品编号:422903
Chemical Name: 6-Amino-2-[3-(cyclopentyloxy)-4-methoxyphenyl]isoindolin-1-one
CAS No. 214071-20-2
项目整合开发状态: Biological Testing
项目研究机构: Daewoong (Originator)
合成路线: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.
📌 参考资料/链接:
参考文献标题:Synthesis and SAR studies for the inhibition of TNF-alpha production.Part 2.2-[3-(Cyclopentyloxy)-4-methoxyphenyl]-substituted-1-isoindolinone derivatives
文献作者:Park,J.S.; Moon,S.C.; Baik,K.U.; Cho,J.Y.; Yoo,E.S.; Byun,Y.S.; Park,M.H.
参考来源:Arch Pharmacal Res 2002,25(2),137