内蒙古师范大学学报(自然科学汉文版)
內矇古師範大學學報(自然科學漢文版)
내몽고사범대학학보(자연과학한문판)
JOURNAL OF INNER MONGOLIA NORMAL UNIVERSITY(NATURAL SCIENCE EDITION)
2015年
4期
477-480
,共4页
程德军%黄斌%李明田
程德軍%黃斌%李明田
정덕군%황빈%리명전
苯磺酰胺%非肽类小分子化合物%生物拮抗剂%1-苯甲基-4-哌啶酮%4-氯苯甲氯
苯磺酰胺%非肽類小分子化閤物%生物拮抗劑%1-苯甲基-4-哌啶酮%4-氯苯甲氯
분광선알%비태류소분자화합물%생물길항제%1-분갑기-4-고정동%4-록분갑록
benzenesulfonamide%non-peptide small molecular compounds%biological antagonists%N-Benzyl-4-piperidone%1-chloro-4-(chloromethyl)benzene
以1-苯甲基-4-哌啶酮合成了4-甲基-N-乙基-N-(4-哌啶基)苯磺酰胺(中间体7),以4-氯苯甲氯为原料,通过溴化及还原合成了5-溴-2-(4-氯苯甲氧基)溴甲基苯(中间体3),通过中间体7和中间体3合成了一种新的小分子化合物4-甲基-N-乙基-N-(N-(5-溴-2-(4-氯苯甲基氧基)苯甲基)-4-哌啶基)苯磺酰胺,对该产物进行了1 H NMR、MS、IR 表征及生物活性检测,结果表明该化合物可以作为药物开发的候选化合物。
以1-苯甲基-4-哌啶酮閤成瞭4-甲基-N-乙基-N-(4-哌啶基)苯磺酰胺(中間體7),以4-氯苯甲氯為原料,通過溴化及還原閤成瞭5-溴-2-(4-氯苯甲氧基)溴甲基苯(中間體3),通過中間體7和中間體3閤成瞭一種新的小分子化閤物4-甲基-N-乙基-N-(N-(5-溴-2-(4-氯苯甲基氧基)苯甲基)-4-哌啶基)苯磺酰胺,對該產物進行瞭1 H NMR、MS、IR 錶徵及生物活性檢測,結果錶明該化閤物可以作為藥物開髮的候選化閤物。
이1-분갑기-4-고정동합성료4-갑기-N-을기-N-(4-고정기)분광선알(중간체7),이4-록분갑록위원료,통과추화급환원합성료5-추-2-(4-록분갑양기)추갑기분(중간체3),통과중간체7화중간체3합성료일충신적소분자화합물4-갑기-N-을기-N-(N-(5-추-2-(4-록분갑기양기)분갑기)-4-고정기)분광선알,대해산물진행료1 H NMR、MS、IR 표정급생물활성검측,결과표명해화합물가이작위약물개발적후선화합물。
Interest in the methylbenzenesulfonamide has been increasing due to pyridine,benzenesulfo-nyl,bromine atom such as active group.The small molecular antagonists can be used as a targeting prepa-ration in the prevention of human HIV-1 infection.4-methyl-N-ethyl-N-(piperidin-4-yl)benzenesulfon-amide(intermediate 7 )was prepared from N-Benzyl-4-piperidone.4-bromo-1-((4-chlorobenzyl)oxy)-2-(bromomethyl)benzene(intermediate 3)was synthesized from 1-chloro-4-(chloromethyl)benzene.Further reaction of 7 with 3 gave a novel compound 4-methyl-N-(1-(5-bromo-2-((4-chlorobenzyl)oxy)benzyl)piper-idin-4-yl)-N-ethylbenzenesulfonamide.The compounds were characterized by 1 H NMR,MS,IR and bioac-tivity.The compound can be used as the candidate compounds for drug development.