Pyriferone, BIM-15427

Chemical Name: 2-Amino-10-fluoro-4,5,6,7-tetrahydro-3H-benzo[6,7]cyclohepta[1,2-d]pyrimidin-4-one
CAS No. 121168-73-8
项目整合开发状态: Preclinical
项目研究机构: Biomeasure (Originator)
合成路线:The nitration of benzosuberone (I) with nitric acid in sulfuric acid gives 3-nitrobenzosuberone (II),which is reacted with ethylene glycol in the presence of p-toluenesulfonic acid yielding 3-nitrobenzosuberone ethylene ketal (III).The catalytic reduction of (III) using Pd/C affords 3-aminobenzosuberone ethylene ketal (IV),which is treated with an aqueous acid to give 3-aminobenzosuberone (V).Diazotization followed by hexafluorophosphoric acid treatment of compound (V) affords diazofluorophosphate complex (VI),which on heating gives 3-fluorobenzosuberone (VII).Carbethoxylation of compound (VII) with diethylcarbonate gives the beta-ketoester (VIII),which is reacted with guanidine carbonate yielding compound (IX).
📌 参考资料/链接:
参考文献标题:Pyriferone
文献作者:Kim,S.H.
参考来源:Drugs Fut 1993,18(11),1009

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