Saterinone, BDF-8634
沙特力农Chemical Name: 1-[4-(3-Cyano-1,2-dihydro-6-methyl-2-oxopyridin-5-yl)phenoxy]-3-[4-(2-methoxyphenyl)piperazin-1-yl]-2-propanol
CAS No. 102669-89-6
项目整合开发状态: Phase II
项目研究机构: Beiersdorf (Originator)
合成路线:The demethylation of 1-(4-methoxyphenyl)acetone (I) by means of AlCl3 gives the corresponding 4-hydroxy compound (III),which is condensed with epichlorohydrin (III),yielding the expected oxiranylmethyl ether (IV).The addition of 1-(2-methoxyphenyl)piperazine (V) to the epoxide ring of (IV) affords the isopropyl alcohol derivative (VI),which is condensed with dimethylformamide dimethylacetal (VII) to afford the dimethylaminobutenone (VIII).Finally,this compound is cyclized with 2-cyanoacetamide (IX) by means of sodium ethoxide,providing the target pyridone.
📌 参考资料/链接：
参考文献标题:Phenylpiperazinylpropanol derivs.
文献作者:(Beiersdorf-Lilly GmbH)
参考来源:DE 3424685; EP 0167121; ES 8608511; JP 1986030573; US 4631279; US 4631281
📄 详细内容
合成路线:The demethylation of 1-(4-methoxyphenyl)acetone (I) by means of AlCl3 gives the corresponding 4-hydroxy compound (III),which is condensed with epichlorohydrin (III),yielding the expected oxiranylmethyl ether (IV).The addition of 1-(2-methoxyphenyl)piperazine (V) to the epoxide ring of (IV) affords the isopropyl alcohol derivative (VI),which is condensed with dimethylformamide dimethylacetal (VII) to afford the dimethylaminobutenone (VIII).Finally,this compound is cyclized with 2-cyanoacetamide (IX) by means of sodium ethoxide,providing the target pyridone.
参考文献标题:SATERINONE (BDF 8634): A DIFFERENT CONCEPT FOR PHARMACOTHERAPY OF CONGESTIVE HEART FAILURE
文献作者:Armah,B.I.; Stenzel,W.
参考来源:Drugs Fut 1989,14(5),445
产品链接: CAS No. 102669-89-6››