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化学学报
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化学学报 ›› 1963, Vol. 29 ›› Issue (4): 260-265. 上一篇    下一篇

论文

5-羥基色胺类似物——Ⅱ.2-甲基-3-(β-氨乙基)-5-甲氧基苯并呋喃及其N-取代衍生物的合成

周启霆, 嵇汝运   

  1. 中国科学院药物研究所
  • 投稿日期:1962-10-31 发布日期:2013-06-03

SEROTONIN ANALOGUES——Ⅱ. THE SYNTHESIS OF 2-METHYL-3-(β-AMINOETHYL)-5-METHOXY-BENZOFURAN AND ITS N-SUBSTITUTED DERIVATIVES

CHOW CHI-TING, KYI ZU-YOONG   

  1. Institute of Materia Medica, Academia Sinica
  • Received:1962-10-31 Published:2013-06-03

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被引次数

1

2-甲基-3-乙酰基-5-羥基苯并呋喃在甲醚化后經Willgerodt-Kindler反应变成N-(2-甲基-5-甲氧基苯并呋喃-3-硫代乙酰)嗎啉(Ⅸ).Ⅸ用碱水解成2-甲基-5-甲氧基苯并呋喃-3-乙酸(Ⅹ)后再变成甲酯(Ⅺ).

It was shown by Shaw and Woolley that in a series of closely related derivatives of serotonin, etherification of the phenolic hydroxyl and introduction of a methyl group in the 2-position favoured the anti-serotonin activity.In the present work, seven derivatives of 3-(β-aminoethyl)-5-β-droxy-berizofuran, an isosteric compound of serotonin, have been synthesized;each of them carries a methyl group on the 2-position and has its 5-hydroxy group methylated, the amino group on the side chain being free or substituted.