化学学报 ›› 1960, Vol. 26 ›› Issue (1): 31-38. 上一篇    下一篇

论文

氨基硫醚及氨基砜化合物的制备

宗汝实, 嵇汝运   

  1. 中国科学院药物研究所
  • 投稿日期:1959-09-29 发布日期:2013-06-03

THE SYNTHESES OF SOME AMINOSULPHIDES AND AMINOSULPHONES

TSUNG JU-SHIH, KYI ZU-YOONG   

  1. Institute of Materia Medica, Academia Sinica, Shanghai
  • Received:1959-09-29 Published:2013-06-03

苄基β-氯乙基硫醚、苯基β-溴乙基硫醚、苄基β-氯乙基砜、苯基β-溴乙基砜分别与各种仲胺作用,制成一系列氨基上有各种不同取代基的β-氨基硫醚及β-氨基砜.有的β-氨基砜则由相应硫醚以过氧化氢氧化制成.二苯甲磺酰乙酸与苯甲醛及醋酸铵共热,除获得预期产物二苯甲基β-氨基-β-苯基乙基砜外,并得副产品二苯甲基β-苯乙烯基砜及二苯甲基甲基砜.苄磺酰乙酸反应时也生成类似产物.二苯甲硫醇与甲醛及仲胺进行Mannich反应,生成预期的氨甲基化产物.

Numerous well-known drugs acting on various nerve systems are phenyl,benzyl or benzhydryl esters,ketones or ethers carrying a β-amino substituted carbon chain. Procaine, Trasentine,Amidone and Benadryl are examples of such types. It appears interesting to see if the corresponding sulphones would also be pharmacologically active. β-Aminosulphones are the oxidation products of the corresponding sulphides. Moreover,the β-aminosulphides could be regarded as the ring-cleaved derivatives of phenothiazine (Ⅰ),and the latter compound is the nucleus of a number of medicinal agents such as promethazine and chlorpromazine. A number of β-aminosulphides and β-aminosulphones are therefore prepared in the present work for pharmacological examinations.