SK&F-94482, BMY-25368

1-氨基-2-[3-(3-哌啶甲基苯氧基)丙丙胺]-1-环丁烯-3,4-二酮一盐酸盐Chemical Name: 1-Amino-2-[3-(3-piperidinomethylphenoxy)propylamino]-1-cyclobutene-3,4-dione monohydrochloride; 3-Amino-4-[[3-[3-(1-piperidinylmethyl)phenoxy]propyl]amino]-3-cyclobutene-1,2-dione monohydrochloride
CAS No. 86134-36-3, 86134-80-7 (free base)
项目整合开发状态: Phase III
项目研究机构: Bristol-Myers Squibb (Originator), GlaxoSmithKline (Licensee)
合成路线:The product is prepared by condensation of 3-[3-(1-piperidinylmethyl)phenoxy]propylamine (I) with 1-amino-2-methoxy-1-cyclobutene-3,4-dione (II) in methanol,followed by treatment with HCl.
📌 参考资料/链接:
参考文献标题:1-Amino-2-[3-(3-piperidinomethylphenoxy)propylamino[cyclobutene-3,4-dione
文献作者:Algieri,A.A.; Crenshaw,R.R.(Bristol-Myers Squibb Co.)
参考来源:DE 3218584; FR 2505835; FR 2513250; GB 2098988; GB 2147899; JP 2036159; US 4390701

📄 详细内容


合成路线:The product is prepared by condensation of 3-[3-(1-piperidinylmethyl)phenoxy]propylamine (I) with 1-amino-2-methoxy-1-cyclobutene-3,4-dione (II) in methanol,followed by treatment with HCl.

参考文献标题:BMY-25368
文献作者:Cavanagh,R.L.
参考来源:Drugs Fut 1985,10(11),890


合成路线:Treatment of 3-amino-4-[3-(3-piperidinomethylphenoxy)propylamino]-1,2,5-thiadiazole-1-oxide,BMY-25260 (I),with an excess of hydrogen chloride in methanol gives N-[3-(3-piperidinomethylphenoxy)propyl]ethanediimidamide trihydrochloride (II) in high yield.Compound (II) is then treated (method A) with sulfur monochloride or sulfur dichloride in DMF,or alternatively (method B) with N,N'-thiobisphthalimide and triethylamine in methylene chloride,followed by treatment with HCl.

合成路线:The product is prepared by condensation of 3-[3-(1-piperidinylmethyl)phenoxy]propylamine (I) with 1-amino-2-methoxy-1-cyclobutene-3,4-dione (II) in methanol,followed by treatment with HCl.
参考文献标题:A novel series of 1-cyclobutene-3,4-dione derivatives with potent and long-acting histamine H2-receptor antagonist activity
文献作者:Luke,G.M.; Standridge,R.T.; Algieri,A.A.; Crenshaw,R.R.; Brown,M.; Partyka,R.A.
参考来源:186th ACS Natl Meet (Aug.28 - Sept.2,Washington,D.C.) 1983,(63),Abst MEDI-63


产品链接: CAS No. 86134-36-3››

产品链接: CAS No.86134-80-7››