新产品编号:108085
Chemical Name: N-[2-[1-[2-(4-Chlorophenoxy)-2-methylpropyl]piperidin-4-yl]-2-methylpropyl]-N,N-dimethylamine difumarate
CAS No. 167710-61-4 (free base), 167710-62-5 (monofumarate)
项目整合开发状态: Biological Testing
项目研究机构: Fournier (Originator)
合成路线:Mannich reaction between 4-isopropylpyridine (I),formaldehyde,and dimethylamine,furnished the pyridyl ethylamine (II).Subsequent hydrogenation of the pyridine ring of (III) in the presence of PtO2 gave rise to piperidine (III).This was coupled with 2-(p-chlorophenoxy)-2-methylpropionic acid (IV) to provide amide (V).Then,amide (V) reduction by means of sodium bis(methoxyethoxy)aluminum hydride produced diamine (VI).This was finally converted to the title maleate salt upon treatment with maleic acid in acetone-ether.
📌 参考资料/链接：
参考文献标题:Derivs.of beta,beta-dimethyl-4-piperidineethanamine as inhibitors of the cholesterol biosynthesis
文献作者:Binet,J.; Samreth,S.; De Fornel,D.(Laboratoires Fournier SA)
参考来源:EP 0699187; FR 2705343; JP 1996510726; US 5614534; WO 9426713
📄 详细内容
合成路线:Mannich reaction between 4-isopropylpyridine (I),formaldehyde,and dimethylamine,furnished the pyridyl ethylamine (II).Subsequent hydrogenation of the pyridine ring of (III) in the presence of PtO2 gave rise to piperidine (III).This was coupled with 2-(p-chlorophenoxy)-2-methylpropionic acid (IV) to provide amide (V).Then,amide (V) reduction by means of sodium bis(methoxyethoxy)aluminum hydride produced diamine (VI).This was finally converted to the title maleate salt upon treatment with maleic acid in acetone-ether.
参考文献标题:Structure activity relationships of new inhibitors of mammalian 2,3-oxidosqualene cyclase designed from isoquinoline derivatives
文献作者:Binet,J.; Thomas,D.; Benmbarek,A.; de Fornel,D.; Renaut,P.
参考来源:Chem Pharm Bull 2002,50(3),316