华西药学杂志
華西藥學雜誌
화서약학잡지
WEST CHINA JOURNAL OF PHARMACEUTICAL SCIENCES
2001年
1期
8-10
,共3页
5-氯-3-(2-噻吩甲酰)-1-甲酰胺-2-羟基吲哚%5-氯-2-羟基吲哚%环氧酶%5-脂化酶%酶抑制剂%非甾体抗炎活性
5-氯-3-(2-噻吩甲酰)-1-甲酰胺-2-羥基吲哚%5-氯-2-羥基吲哚%環氧酶%5-脂化酶%酶抑製劑%非甾體抗炎活性
5-록-3-(2-새분갑선)-1-갑선알-2-간기신타%5-록-2-간기신타%배양매%5-지화매%매억제제%비치체항염활성
目的：合成具抗炎活性的5-氯-3-（2-噻吩甲酰）-1-甲酰胺-2-羟基吲哚钠盐。方法：以对氯苯胺为起始原料，经四步反应制得关键中间体5-氯-2-羟基吲哚，收率75%，然后与三氯乙酰异腈酸酯和2-噻吩甲酰氯反应，最后经NaHCO3处理，制得标题化合物。结果：总收率可达45%以上，标题化合物经红外光谱、核磁共振谱、质谱及元素分析确证了结构。结论：该实验方法条件温和，操作简单，收率高，适合大规模合成。
目的：閤成具抗炎活性的5-氯-3-（2-噻吩甲酰）-1-甲酰胺-2-羥基吲哚鈉鹽。方法：以對氯苯胺為起始原料，經四步反應製得關鍵中間體5-氯-2-羥基吲哚，收率75%，然後與三氯乙酰異腈痠酯和2-噻吩甲酰氯反應，最後經NaHCO3處理，製得標題化閤物。結果：總收率可達45%以上，標題化閤物經紅外光譜、覈磁共振譜、質譜及元素分析確證瞭結構。結論：該實驗方法條件溫和，操作簡單，收率高，適閤大規模閤成。
목적：합성구항염활성적5-록-3-（2-새분갑선）-1-갑선알-2-간기신타납염。방법：이대록분알위기시원료，경사보반응제득관건중간체5-록-2-간기신타，수솔75%，연후여삼록을선이정산지화2-새분갑선록반응，최후경NaHCO3처리，제득표제화합물。결과：총수솔가체45%이상，표제화합물경홍외광보、핵자공진보、질보급원소분석학증료결구。결론：해실험방법조건온화，조작간단，수솔고，괄합대규모합성。
OBJECTIVE:A facile synthesis of sodium salt of 5-chloro-3-(2-thenoyl)-2-oxindole-1-carboxyamide from common 4-chloroaniline is described.METHODS:The key intermediate 5-chloro-2-oxindole(4) is prepared successfully in 75% yield from 4-chloroaniline in four steps, and converted by reaction with trichloroacetyl isocyanate into the N-trichloroacetyl-5-chloro-2-oxindole-1-carboxyamide,and followed hydrolysis, then 5-chloro-2-oxindole-1-carboxyamide(5) is obtained. Condensation of (5) with 2-thenoyl chloride gives 5-chloro-3-(2-thenoyl)- 2-oxindole-carboxyamide(6). The title compound is obtained by treating(6) with NaHCO3.RESULTS:The title compound is prepared successfully over 45% yield. The structure is characterized by elementary analysis,IR,MS,1H NMR,H-H COSY,13C NMR ,DEPT and HMQC. CONCLUSION:The method is simple and applicable to large scale preparation
