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SYNTHESIS OF ESTERS OF 2-CHLOROMETHYL-6-METHYLBENZOIC ACID

机译:2-氯-6-甲基苯甲酸的酯的合成

摘要

FIELD: chemistry.;SUBSTANCE: present invention pertains to new compounds with formula , in which R represents H, (C1-C12)-alkyl or (C1-C4)-alkyl-(C6-C12)-aryl. In the alkyl, one or more CH2-groups can be substituted with -O-. The invention also relates to the method of obtaining these compounds. The method involves reacting dimethylbenzoic acid ester with formula where R assumes values given above, with a chlorinating agent in an inert solvent or without a solvent at temperature above 40C, and then cleaning, if necessary. Formula (I) compounds are essential intermediate products during synthesis of PPAR agonists with formula , in which R represents H, (C1-C12)-alkyl or (C1-C4)-alkyl-(C6-C12)-aryl. In the alkyl, one or more CH2-groups can be substituted with -O-; Y represents -(CH2)3-, 1,3-phenylene, 1,3-cyclohexanediyl; R' represents H, F, Br, CF3, (C1-C6)-alkyl, O-(C1-C6)-alkyl, phenyl; CF3; obtained from reaction of compounds with formula with formula (I) compounds in toluene, N-methylpyrrolidone or other aprotic solvents, in the presence of a suitable base, at temperature lying in the -78C - +50C interval, with subsequent extractive processing and, if necessary, crystallisation of the end product.;EFFECT: obtaining new compounds.;8 cl, 5 ex
机译:技术领域本发明涉及具有式<图像文件=“ 00000005.GIF” he =“ 36” imgContent =“ undefined” imgFormat =“ GIF” wi =“ 36” />的新化合物,其中R代表H,(C 1 -C 12 )-烷基或(C 1 -C 4 )-烷基-(C 6 -C 12 )-芳基。在烷基中,一个或多个CH 2 -基团可以被-O-取代。本发明还涉及获得这些化合物的方法。该方法包括使二甲基苯甲酸酯与式进行反应,其中R表示以上给出的值,并进行氯化处理在惰性溶剂中或在无溶剂的情况下在高于40℃的温度下使用抗氧化剂,然后根据需要进行清洁。式(I)化合物是合成式为<图像文件=“ 00000007.GIF” he =“ 54” imgContent =“ undefined” imgFormat =“ GIF” wi =“ 90” />的PPAR激动剂期间必不可少的中间产物,其中R代表H,(C 1 -C 12 )-烷基或(C 1 -C 4 )-烷基-(C 6 -C 12 )-芳基。在烷基中,一个或多个CH 2 -基团可以被-O-取代; Y代表-(CH 2 3 -,1,3-亚苯基,1,3-环己二基; R'代表H,F,Br,CF 3 ,(C 1 -C 6 )-烷基,O-(C 1 -C 6 )-烷基,苯基; CF 3 ;从具有式与式(I)化合物在甲苯中合成,N-甲基吡咯烷酮在合适的碱存在下,于-78°C-+ 50°C的温度范围内进行加热或其他非质子溶剂,随后进行萃取过程和最终产物的结晶(必要时进行结晶);效果:获得新化合物。; 8 cl ,5前

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