【药物名称】SCH-79797
化学结构式(Chemical Structure):
参考文献No.545768
标题:Structure-activity relationships of pyrroloquinazolines as thrombin receptor antagonists
作者:Ahn, H.-S.; Arik, L.; Boykow, G.; Burnett, D.A.; Caplen, M.A.; Czarniecki, M.; Domalski, M.S.; Foster, C.; Manna, M.; Stamford, A.W.; Wu,Y.
来源:Bioorg Med Chem Lett 1999,9(14),2073
合成路线图解说明:

Alkylation of 5-nitroindole (I) with 4-isopropylbenzyl chloride (II) in the presence of Cs2CO3 provided the N-benzylindole derivative (III). Reduction of the nitro group of (III) by hydrogenation over Pd/C gave the corresponding amine, which was isolated as the hydrochloride salt (IV). The required pyrroloquinazoline system (V) was then prepared by reaction of (IV) with trichloromethyl isocyanate, followed by treatment with POCl3. Displacement of the 1-chlorine of (V) by ammonia afforded amine (VI). The remaining 3-chlorine of (VI) was then displaced by cyclopropylamine (VII) to furnish the title compound.

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