42864-78-8
42864-78-8 結(jié)構(gòu)式
基本信息
鹽酸貝凡洛爾
貝凡洛爾鹽酸鹽
1-[[2-(3,4-二甲氧苯基)乙基]氨基]-3-(3-甲基苯氧基)-2-丙醇鹽酸鹽
CI 775
Vantol
NC 1400
Sentiloc
Ranestol
BEVANTOLOL HCL
NC-1400 hydrochloride
bevantolol hydrochloride
Bevantolol hydrochloride 1-5 g
物理化學(xué)性質(zhì)
常見問題列表
pKi: 7.83 (β1-adrenergic receptor), 6.9 (α1-adrenergic receptor), 6.23 (β2-adrenergic receptor) and Ca 2+
Bevantolol hydrochloride has a pK i of 6.23 for β2-adrenergic receptor.
2186-25-6
120-20-7
42864-78-8
該化合物通過類似于先前文獻(xiàn)報道的方法制備。將外消旋的1,2-環(huán)氧-3-(3-甲基苯氧基)丙烷(rac-2, 21.0 g, 0.128 mol)與3,4-二甲氧基苯乙胺(23.2 g, 0.128 mol)在50 mL乙醇中于25-30°C下攪拌反應(yīng)24小時。反應(yīng)進(jìn)程通過薄層色譜(TLC)進(jìn)行監(jiān)測。待起始環(huán)氧化物完全消耗后，將反應(yīng)混合物減壓濃縮至干，殘余物溶于乙酸乙酯(EtOAc)中，通入氣態(tài)氯化氫(HCl)至溶液飽和，得到37.5 g (75%產(chǎn)率)粗產(chǎn)物rac-1·HCl。該粗產(chǎn)物經(jīng)乙腈/乙醇(CH3CN/EtOH, 9:1 v/v)混合溶劑重結(jié)晶后，得到26.4 g (54%產(chǎn)率)純品rac-1·HCl，為白色固體，熔點(diǎn)140-141°C。1H NMR (δ): 2.29 (s, 3H, CH3), 3.21-3.37 (m, 6H, CH2N + CH2CH2), 3.84 (s, 3H, OCH3), 3.85 (s, 3H, OCH3), 3.97 (dd, J = 9.7, 5.9 Hz, 1H, OCH2), 4.06 (dd, J = 9.7, 4.3 Hz, 1H, OCH2), 4.69 (m, 1H, OCH), 5.26 (br s, OH), 6.63-6.67 (m, 2H, Ar), 6.76-6.81 (m, 4H, Ar), 7.12 (t, J = 7.8 Hz, 1H, Ar), 8.90 (br s, N+H), 9.80 (br s, 1H, N+H)。
參考文獻(xiàn)：
[1] Tetrahedron Asymmetry, 2016, vol. 27, # 9-10, p. 397 - 403
[2] Journal of Molecular Structure, 2009, vol. 936, # 1-3, p. 171 - 176
Bevantolol hydrochloride (200 mg/kg; PO by water; for 6 weeks) produces a significant decrease in the expression level of β1 adrenoceptor mRNA.
| Animal Model: | Male Wistar rats weighing 250-300 g |
| Dosage: | 200 mg/kg |
| Administration: | PO by water; for 6 weeks |
| Result: | Produced a significant decrease in the expression level of β1 adrenoceptor mRNA. |