孙存济, 陸顺兴, 嵇汝运. 延胡索乙素(四氢巴马亭)有关化合物的合成——Ⅳ.酰氧基和烷氧基小蘖因的合成J. 药学学报, 1965, 12(5): 314-318.
引用本文: 孙存济, 陸顺兴, 嵇汝运. 延胡索乙素(四氢巴马亭)有关化合物的合成——Ⅳ.酰氧基和烷氧基小蘖因的合成J. 药学学报, 1965, 12(5): 314-318.
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SUN TSUN-TSI, LOH SHEUN-HSING AND KYI ZU-YOONG, . SYNTHESIS OF COMPOUNDS RELATED TO CORYDALIS B (TETRAHYDROPALMATINE) Ⅳ. THE SYNTHESIS OF SOME ACYLOXY AND ALKOXY BERBINESJ. Acta Pharmaceutica Sinica, 1965, 12(5): 314-318.
Citation: SUN TSUN-TSI, LOH SHEUN-HSING AND KYI ZU-YOONG, . SYNTHESIS OF COMPOUNDS RELATED TO CORYDALIS B (TETRAHYDROPALMATINE) Ⅳ. THE SYNTHESIS OF SOME ACYLOXY AND ALKOXY BERBINESJ. Acta Pharmaceutica Sinica, 1965, 12(5): 314-318.
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延胡索乙素(四氢巴马亭)有关化合物的合成——Ⅳ.酰氧基和烷氧基小蘖因的合成

SYNTHESIS OF COMPOUNDS RELATED TO CORYDALIS B (TETRAHYDROPALMATINE) Ⅳ. THE SYNTHESIS OF SOME ACYLOXY AND ALKOXY BERBINES

    摘要
  • 摘要: 延胡索乙素2,3-和9-的三个甲氧基及四氢小檗碱的9-甲氧基分别换以乙氧基及各种酰氧基,制得11个类似物.又分别合成了2,3-二羟基与2,3-次甲二氧基-9,10-二甲氧基小蘖因的氯丁烷与丁撑二溴季铵盐.合成的化合物经药理试验表明其中乙氧基及酰氧基小蘖因虽保留延胡索乙素的镇痛和镇静作用,但它们的作用强度大都减弱.

     

    Abstract: Eleven analogues of Corydalis B (tetrahydropalmatine) were prepared by acylation and ethylation of the hydroxyberbines derived from berberine and palmatine under vari- ous conditions. Alkylation with butyl bromide in the presence of potassium carbonate gave the unexpected quaternary ammonium salt. Pharmacological examinations revealed that some of these compounds (Ⅰ, Ⅱ) had analgesic and sedative activities less potent than those of Corydalis B.

     

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