Ibudilast, KC-404, Eyevinal(Ophthalmic), Ketas
异丁司特Chemical Name: 3-Isobutyryl-2-isopropylpyrazolo[1,5-a]pyridine; 1-(2-Isopropylpyrazolo[1,5-a]pyridin-3-yl)-2-methyl-1-propanone
CAS No. 50847-11-5
项目整合开发状态: Launched-1989
项目研究机构: Kyorin (Originator), Banyu (Licensee), MediciNova (Licensee)
合成路线:By condensation of 1-amino-2-methylpyridinium iodide (I) with isobutyric anhydride (II) by means of K2CO3 at reflux temperature.
📌 参考资料/链接：
参考文献标题:2-Alkyl-3-acylpyrazolo[1,5-a]pyridines
文献作者:Irikura,T.; et al.(Kyorin Pharmaceutical Co.,Ltd.)
参考来源:DE 2315801; FR 2182914; JP 7714799
📄 详细内容
合成路线:By condensation of 1-amino-2-methylpyridinium iodide (I) with isobutyric anhydride (II) by means of K2CO3 at reflux temperature.
合成路线:The reaction of 6-(4-phenylbutoxy)hexanol methanesulfonate (I) with (R)-phenylglycinol (II) by means of DIEA and NaI in hot acetonitrile gives the secondary amine (III),which is condensed with 2-(benzyloxy)-5-(2-bromoacetyl)benzoic acid methyl ester (IV) by means of DIEA in refluxing 1,2-dimethoxyethane to yield the tertiary amine (V).The enantioselective reduction of (V) with LiBH4 in refluxing dimethoxyethane affords the tetrahydroxy derivative (VI),which is finally debenzylated by hydrogenation with H2 over Pd/C in ethanol to provide the target aminoethanol derivative.
参考文献标题:A novel process for preparing salmeterol
文献作者:Procopiou,P.A.(GlaxoSmithKline plc)
参考来源:WO 0196278
产品链接: CAS No. 50847-11-5››