CAS: 27913-99-1; 4-(4-Methylpiperazin-1-yl)Benzaldehyde

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CAS号109-01-3 N-甲基哌嗪 | CAS号459-57-4 对氟苯甲醛 | CAS号342405-34-9 4-(4-甲基哌嗪)苄醇 | CAS号61568-51-2 1-溴-4-(1,3-二噁烷-2-基)苯 | CAS号34334-28-6 4-(4-甲基-1-哌嗪基)苯腈 | CAS号3074-43-9 1-甲基-4-苯基哌嗪 | CAS号68104-63-2 4-(1-哌嗪基)苯腈 | CAS号197638-83-8 1-B°C-4-(4-甲酰苯基)哌嗪 | CAS号342405-34-9 4-(4-甲基哌嗪)苄醇 | CAS号1095382-05-0 3-[[4-[6-溴-2-[4... | CAS号505-20-4 1,2-dithiane

4-哌嗪基苯甲腈置于三乙酰氧基硼氢化钠,二异丁基氢化铝,溶剂黄146体系中,用 正己烷,二氯甲烷,甲苯 用作溶剂,化学反应 12.5H,反应生成4-(4-甲基哌嗪)苯甲醛
参考文献:合成具有5,11-二氢-6H-吡啶并[2,3-B] [1,4]苯并二氮杂-6-骨架作为有效和选择性的m2毒蕈碱受体拮抗剂的新型琥珀酰胺衍生物.二.
标题:合成具有5,11-二氢-6H-吡啶并[2,3-B] [1,4]苯并二氮杂-6-骨架作为有效和选择性的m2毒蕈碱受体拮抗剂的新型琥珀酰胺衍生物.二.
摘要:制备了一系列含有5,11-二氢-6H-吡啶并[2,3-B] [1,4]苯并二氮杂-6-6骨架(6A-Z)的琥珀酰胺衍生物,并评估了其与毒蕈碱受体的结合亲和力.与af-Dx 116(1A)相比在体外以及对心动过缓和体内唾液的拮抗作用.体外结构-活性关系(sar)研究表明,4-(4-烷基-1-哌嗪基)苄氨基部分在增强与m2毒蕈碱受体的亲和力中起关键作用.含有4-(4-异丙基-1-哌嗪基)苄基甲基氨基的化合物6Y对m2毒蕈碱受体的亲和力最高(pki = 9.2),效力是1A的200倍,而化合物6U含有4-(与m3毒蕈碱受体相比,4-乙基-1-哌嗪基)苄基乙基氨基部分显示出最高的m2选择性(m3 / M2比= 320).静脉或口服给药后,6Y和6U均能拮抗氧代雷斯莫林诱导的大鼠心动过缓.有意识的狗的口服评估表明,提高心率的功效至少是1A的3倍.
Doi:10.1248/cpb.45.1458

专利信息

专利号:US-9701686-B2
优先权日:2009-12-04
标题:Tricyclopyrazole derivatives
发明人：DISINGRINI TERESA; MANTEGANI SERGIO; VARASI MARIO
权利人:NERVIANO MEDICAL SCIENCES SRL
摘要:Compounds which are tricyclopyrazole derivatives or pharmaceutically acceptable salts thereof, their preparation process and pharmaceutical compositions comprising them are disclosed; these compounds are useful in the treatment of diseases caused by and/or associated with an altered protein kinase activity such as cancer, viral infection, prevention of AIDS development in HIV-infected individuals, cell proliferative disorders, autoimmune and neurodegenerative disorders; also disclosed is a process under Solid Phase Synthesis conditions for preparing the compounds of the invention and chemical libraries comprising a plurality of them.