39552-01-7
39552-01-7 结构式
基本信息
中文别名
苯呋洛尔2-乙酰-7-(2-羟基-3-异丙胺丙氧)-苯并呋喃
英文别名
Befunolol2-acetyl-7-(2-hyroxy-3-isopropylaminopropoxy)benzofuran
2-Acetyl-7-(2-hydroxy-3-isopropylaminopropoxy)benzofuran
(-)-2-Acetyl-7-[(S)-2-hydroxy-3-isopropylaminopropoxy]benzofuran
(+)-2-Acetyl-7-[(R)-2-hydroxy-3-isopropylaminopropoxy]benzofuran
7-(2-hydroxy-3-(isopropylamino)propoxy)-2-benzofuranyl methyl ketone
ketone, 7-(2-hydroxy-3-(isopropylamino)propoxy)-2-benzofuranyl methyl
7-[2-Hydroxy-3-(iso-propylamino)propoxy]-2-benzofuranyl methyl ketone
1-(7-(2-hydroxy-3-((1-methylethyl)amino)propoxy)-2-benzofuranyl)ethanone
1-(7-(2-hydroxy-3-((1-methylethyl)amino)propoxy)-2-benzofuranyl)-ethanon
所属类别
原料药：抗心律失常药物理化学性质
外观性状结晶。熔点115℃。苯呋洛尔盐酸盐（C16H21NO4·HCI)，熔点163℃。
熔点115°
沸点433.35°C (rough estimate)
密度1.1049 (rough estimate)
折射率1.5500 (estimate)
储存条件Hygroscopic, -20°C Freezer, Under inert atmosphere
溶解度氯仿（微溶）、DMSO（微溶、加热）
形态固体
颜色白色至灰白色
CAS 数据库39552-01-7
制备方法
方法1
由2-乙酰-7-羟基苯并呋喃与3-氯-1,2-环氧丙烷反应后再与异丙胺作用而得。取8.8g2-乙酰-7-羟基苯并呋喃中，加入80ml3-氯-1,2-环氧丙烷和0.2g盐酸哌啶。将混合物加热至105℃，反应3h。反应后蒸发出过量的3-氯-1,2-环氧丙烷。生成物在减压下蒸馏，得9.3g2-乙酰-7-（2,3-环氧丙氧）苯并呋喃，沸点175-176℃（93Pa）。取6g上述生成物溶于30ml乙醇中，加10ml异丙胺，混合物回流40min，由反应混合物中蒸除溶剂，得到的残余物用环己烷-丙酮重结晶，得6g苯呋洛尔。常见问题列表
生物活性
(±)-Befunolol 是一种 β-肾上腺素能受体阻断剂。靶点
Adrenoreceptor
体外研究
A β-adrenoceptor blocking agent, Befunolol, is found to has intrinsic sympathomimetic activities in isolated right atria, trachea and taenia caecum of guinea pig (intrinsic activities are 0.22-0.28). The pD2-values of Befunolol estimated in the isolated organs are significantly different from its pA2-values against isoprenaline. Befunolol interacts with the beta-adrenoceptor where there may be two different sites: one site for agonistic action and the other for competitive antagonistic action. The intrinsic activity of Befunolol may be equal to its selectivity for both the sites.