MR-20494
Chemical Name: 6-(4-Chlorophenyl)-7-[3-pyridinylmethylene]-5,6,7,8-tetrahydroindolizin-8-one
项目整合开发状态: Biological Testing
项目研究机构: CNRS (Originator), Universit?de Caen (Originator)
合成路线:The cyclization of the amino group of 4-amino-3-(4-chlorophenyl)butyric acid (I) with 2,5-dimethoxytetrahydrofuran (II) by means of AcOH in THF gives the corresponding pyrrole (III),which is cyclized by means of TEA,ClCOOEt,pyrrolidine and POCl3 in toluene yielding the pyrrolopyridone (IV).Finally,this compound is condensed with pyridine-4-carbaldehyde (V) by means of tetrabutylammonium bisulfate and NaOH in water.
合成路线:The cyclization of the amino group of 4-amino-3-(4-chlorophenyl)butyric acid (I) with 2,5-dimethoxytetrahydrofuran (II) by means of AcOH in THF gives the corresponding pyrrole (III),which is cyclized by means of TEA,ClCOOEt,pyrrolidine and POCl3 in toluene yielding the pyrrolopyridone (IV).Finally,this compound is condensed with pyridine-3-carbaldehyde (V) by means of tetrabutylammonium bisulfate and NaOH in water.
📌 参考资料/链接:
参考文献标题:MR 20492 and MR 20494: Two indolizinone derivatives that strongly inhibit human aromatase
文献作者:Auvray,P.; Sourdaine,P.; Moslemi,S.; S閞alini,G.-E.; Sonnet,P.; Enguehard,C.; Guillon,J.; Dallemagne,P.; Bureau,R.; Rault,S.
参考来源:J Steroid Biochem Mol Biol 1999,70(1-3),59