首页> 外国专利> A PROCESS FOR SYNTHESIS OF 1-ARYL-3-ARYL/HETEROARYL-3-ARYLTHIO/HETEROARYLTHIO-1-PROPANONES POSSESSING ANTIFUNGAL ACTIVITY

A PROCESS FOR SYNTHESIS OF 1-ARYL-3-ARYL/HETEROARYL-3-ARYLTHIO/HETEROARYLTHIO-1-PROPANONES POSSESSING ANTIFUNGAL ACTIVITY

机译:具有抗真菌活性的1-aryl-3-aryl / heteroaryl-3-arylthio / heterarylthio-1-propaneones的合成方法

摘要

A process for synthesis of compounds 1- aryl-3-aryl / heteroaryl-3-arylthio / heteroarylthio-1-propanones, of formula (F-l), possessing antifungal activity, wherein, R1 is selected from H, OH; R2 is selected from H, OH, OCH3, CI, NO2; Ar2 is selected from H, Phenyl; Ar1 is selected from compounds of formula (F-IV) or (F- V) wherein, R3 is selected from -H, -NO2; Ar3 is selected from compounds of formula (F - VI) or (F- VII) wherein, R4 is selected from H, -NHCOCH3; the said process comprising, a. reacting a compound of Formula (F-ll) wherein, R1, R2, Ar1 and Ar2 are same as in Formula (F-l) with a compound of Formula (F-lll) wherein, Ar3 is same as in Formula (F-l) in a basic medium using bases such as triethylamine, pyridine, alkoxides such as sodium methoxide, sodium ethoxide, in an organic solvent selected from group comprising chlorinated solvents such as chloroform, dichloromethane, carbon tetrachloride, aromatic hydrocarbons such as benzene, toluene, esters such as ethyl acetate and ketones such as methyl isobutyl ketone; b. removing the solvent after the reaction and taking the dry product in water and extracting the reaction product in aqueous solution with another organic solvent which may be same or different but selected from group as in step (a), c. removing the solvent from the extract; and d. further purifying the product obtained at stage c, using silica gel column chromatography.
机译:具有抗真菌活性的式(F-1)的式(F-1)的化合物1-芳基-3-芳基/杂芳基-3-芳硫基/杂芳硫基-1-丙烷的合成方法,其中,R 1选自H,OH; R 2选自H,OH,OCH 3,Cl,NO 2; Ar 2选自H,苯基; Ar 1选自式(F-IV)或(F-V)的化合物,其中,R 3选自-H,-NO 2; Ar 3选自式(F-VI)或(F-VII)的化合物,其中,R 4选自H,-NHCOCH 3;所述过程包括:a。使其中R 1,R 2,Ar 1和Ar 2与式(F1)相同的式(F-II)化合物与其中Ar 3与式(F1)相同的式(F-III)化合物反应在选自包括氯仿,二氯甲烷,四氯化碳等氯代溶剂,苯​​,甲苯等芳香烃,乙基等酯的氯溶剂的有机溶剂中使用三乙胺,吡啶,醇盐如甲醇钠,乙醇钠等碱的碱性介质乙酸酯和酮,例如甲基异丁基酮; b。反应后除去溶剂,将干燥产物溶于水中,再用另一种有机溶剂萃取反应产物,该有机溶剂可以相同或不同,但选自步骤(a),c中。从提取物中除去溶剂; d。使用硅胶柱色谱法进一步纯化在步骤c中获得的产物。

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