Nipradolol, Nipradilol, KT-210, K-351, Nipranol, Hypadil

尼普地洛Chemical Name: 3,4-Dihydro-8-(2-hydroxy-3-isopropylaminopropoxy)-3-nitroxy-2H-1-benzopyran; 3,4-Dihydro-8-[2-hydroxy-3-[(1-methylethyl)amino]propoxy]-2H-1-benzopyran-3-ol 3-nitrate
CAS No. 81486-22-8
项目整合开发状态: Launched-1988
项目研究机构: Kowa (Originator), Orion Pharma (Licensee)
合成路线:The reaction of 3,4-dihydro-2H-1-benzopyran-3,8-diol (I) with ethyl chloroformate by means of triethylamine in THF gives 3,4-dihydro-8-lethoxy carbonyloxyl-2H-1-benzopyran-3-ol (II),which is treated with nitric acid and acetic anhydride in acetonitrile to yield 3,4-dihydro-8-(ethoxycarbonyloxy)-2H-1-benzopyran-3-ol-3-nitrate (III).The hydrolysis of (III) with NaOH in methanol affords 3,4-dihydro-8-hydroxy-2H-1-benzopyran-3-ol 3-nitrate (IV),which is condensed with epichlorohydrin (V) by means of NaOH in water giving 3,4-dihydro-8-(2,3-epoxypropoxy)-2H-1-benzopyran-3-ol 3-nitrate (VI).Finally,this compound is treated with isopropylamine in refluxing ethanol.