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新腎上腺素能β-受体阻断剂6-(2-异丙氨基-1-羟基乙基)-1,4-苯并二氧己环的合成
引用本文:陈志豪,嵇汝运. 新腎上腺素能β-受体阻断剂6-(2-异丙氨基-1-羟基乙基)-1,4-苯并二氧己环的合成[J]. 药学学报, 1965, 12(9): 623-624
作者姓名:陈志豪  嵇汝运
作者单位:中国科学院药物研究所,上海
摘    要:Bromination of 6-acetyl-1,4-benzodioxane gave 6-(α-bromoacetyl)-1,4-benzodioxane (IVb), which was condensed with isopropylamine, forming 6-(α-isopropylaminoacetyl)- 1,4-benzodioxane (IVc). The latter compound afforded the desired aminoethanol (III) upon reduction with potassium borohydride.Pharmacological examinations revealed that III was more potent in adrenergic beta-blocking effect, but was less toxic in comparison with pronethalol.

收稿时间:1965-03-01

THE SYNTHESIS OF A NEW ADRENERGIC BETA-RECEPTORBLOCKING AGENT 6-(2-ISOPROPYLAMINO-1-HYDROXYETHYL)-1,4-BENZODIOXANE
CHEN CHI-HAO KYI ZU-YOONG. THE SYNTHESIS OF A NEW ADRENERGIC BETA-RECEPTORBLOCKING AGENT 6-(2-ISOPROPYLAMINO-1-HYDROXYETHYL)-1,4-BENZODIOXANE[J]. Acta pharmaceutica Sinica, 1965, 12(9): 623-624
Authors:CHEN CHI-HAO KYI ZU-YOONG
Abstract:Bromination of 6-acetyl-1,4-benzodioxane gave 6-(α-bromoacetyl)-1,4-benzodioxane (IVb), which was condensed with isopropylamine, forming 6-(α-isopropylaminoacetyl)- 1,4-benzodioxane (IVc). The latter compound afforded the desired aminoethanol (III) upon reduction with potassium borohydride.Pharmacological examinations revealed that III was more potent in adrenergic beta-blocking effect, but was less toxic in comparison with pronethalol.
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