有机化学
有機化學
유궤화학
CHINESE JOURNAL OF ORGANIC CHEMISTRY
2009年
7期
1161-1164
,共4页
习保民%江振洲%王涛%倪沛洲
習保民%江振洲%王濤%倪沛洲
습보민%강진주%왕도%예패주
磺酰胺%合成%α1-肾上腺素受体拮抗剂
磺酰胺%閤成%α1-腎上腺素受體拮抗劑
광선알%합성%α1-신상선소수체길항제
sulfonamide%synthesis%α1-adrenoceptor antagonist
7-氨基乙基-(3,4-二氢-2H-苯并[1,2]噻嗪-1,1-二氧代)盐酸盐和取代苯氧丙-2-酮经还原胺化,合成了10个新的环状胺磺酰基取代的苯乙胺和苯氧烷胺类化合物.化合物经1H NMR,HRMS,IR确证其结构.生物活性测试结果表明,所有化合物对α1-肾上腺素受体均具有一定的拮抗作用.
7-氨基乙基-(3,4-二氫-2H-苯併[1,2]噻嗪-1,1-二氧代)鹽痠鹽和取代苯氧丙-2-酮經還原胺化,閤成瞭10箇新的環狀胺磺酰基取代的苯乙胺和苯氧烷胺類化閤物.化閤物經1H NMR,HRMS,IR確證其結構.生物活性測試結果錶明,所有化閤物對α1-腎上腺素受體均具有一定的拮抗作用.
7-안기을기-(3,4-이경-2H-분병[1,2]새진-1,1-이양대)염산염화취대분양병-2-동경환원알화,합성료10개신적배상알광선기취대적분을알화분양완알류화합물.화합물경1H NMR,HRMS,IR학증기결구.생물활성측시결과표명,소유화합물대α1-신상선소수체균구유일정적길항작용.
A series of novel cyclosulfamido substituted phenoxylalkylamine derivatives were synthesized through the condensation and reduction of various substituted phenoxypropan-2-one with 7-(2-aminoethyl-3,4-dihydro-1,1-dioxo-2H-benzo[e][1,2]thiazine)hydroeholoride (5). Their structures were identified by 1H NMR, HRMS, and IR data. The target compounds have been assayed with function analysis in anococeyeus muscle, indicating that all of them have good blocking activity to α1-adrenoceptor.