新产品编号:1414817
Chemical Name: 7(R)-Isopropyl-5-methyl-2-(4-methylpentyl)-4,5,7,8-tetrahydro-3H-imidazo[2,1-b]purin-4-one
项目整合开发状态: Biological Testing
项目研究机构: Schering-Plough (Originator)
合成路线:The acylation of 6-amino-5-(benzylamino)-2-methylpyrimidine-2,4(1H,3H)-dione (I) with 5-methylhexanoic acid (II) by means of EDCI and DMAP gives the amide (III),which is cyclized by means of hot POCl3 affording the chloropurin-6-one (IV).The condensation of (IV) with the chiral aminoalcohol (V) by means of DIEA and NMP yields intermediate (VI),which is cyclized by means of SOCl2 in dichloromethane providing the imidazo-purine (VII).Finally,this compound is debenzylated with ammonium formate and Pd(OH)2.
📌 参考资料/链接:
参考文献标题:Synthesis and evaluation of potent and selective c-GMP phosphodiesterase inhibitors
文献作者:Ho,G.D.; Silverman,L.; Bercovivi,A.; Puchalski,C.; Tulshian,D.; Xia,Y.; Czarniecki,M.; Green,M.; Cleven,R.; Zhang,H.; Fawzi,A.
参考来源:Bioorg Med Chem Lett 1999,9(1),7