CAS: 38487-86-4; 2-Amino-4-Chlorobenzonitrile

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2-氨基-4-氯苯甲酰胺置于potassium Carbonate,三乙胺,三氟乙酸酐体系中,化学反应生成2-氨基-4-氯苯腈
参考文献:4-取代-3-苯基喹啉-2(1H)-Ones:具有体内活性的酸性和非酸性甘氨酸位点n-甲基-D-天冬氨酸拮抗剂.
标题:4-取代-3-苯基喹啉-2(1H)-Ones:具有体内活性的酸性和非酸性甘氨酸位点n-甲基-D-天冬氨酸拮抗剂.
摘要:合成了4-取代的3-苯基喹啉-2(1H)-Ones,并在体外评估了nmda(n-甲基-D-天冬氨酸)受体甘氨酸位点的拮抗剂活性,并在体内评估了dba中的抗惊厥活性.在音源性癫痫发作模型中为小鼠的/ 2品系.4-氨基-3-苯基喹啉-2(1H)-一(3)的结合亲和力比酸性4-羟基化合物1低40倍,但作为抗惊厥剂仅弱4倍.图3给出了一种酸性化合物(6,Pka = 6.0),其亲和力被完全恢复,但体内效力却显着降低(表1).1的4位甲基化可得到18个结果,从而消除了可测量的亲和力,但是,中性氢键接受基团与18的甲基相连会产生具有与1相当的体外和体内活性的化合物(例如,表2中的23和28).用乙基取代1的4-羟基可消除活性(42),但再次,将中性氢键受体结合到末端碳原子上可恢复亲和力(例如,表3中的36,39和40).用氨基取代高亲和力化合物2的4-羟基会产生亲和力降低200倍的化合物(43; Ic50
Doi:10.1021/jm9605492

专利信息

专利号:US-4257942-A
优先权日:1977-10-06
标题:New water-insoluble azo dyes
发明人：DEFEO FRANCESCO; CIPOLLI ROBERTO
权利人:ACNA
摘要:The present invention relates to the synthesis of new dyes having the following general formula: wherein: D is the residue of a diazotizable component of the carbocyclic or heterocyclic series X is an ethylene group, optionally substituted by halogen-methyl, alkyl C1-C4, aryl, aralkyl or CH2OCO(HN)nR (wherein R and n have the meanings hereinafter defined); R is alkyl C1-C8 optionally substituted by halogen, CN,COOH; aryl optionally substituted by one or more atoms of halogen, alkyl C1-C4, alkoxyl C1-C4; alkoxyl C1-C4; alkoxyl C1-C8; Aryloxy; aralkoxy; cycloalkoxy; aralkyl; naphthyl optionally substituted by halogen; alkenyl C2-C8, optionally substituted by halogen, CN, COOH; R1 and R2, either like or unlike each other, may be alkyl C1-C4 optionally substituted by halogen or CN groups; aralkyl; R3 is H; halogen, alkyl C1-C4; alkoxyl C1-C4, optionally substituted. n is 0 or 1.