CAS: 120511-74-2; 2,2'-(5-Methyl-1,3-Phenylene)Diacetonitrile

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CAS号19294-04-3 3,5-二(溴甲基)甲苯 | CAS号143-33-9 氰化钠 | CAS号151-50-8 氰化钾 | CAS号64-17-5 乙醇 | CAS号120511-72-0 5,α,α,α',α'-五甲基...

3,5-二(溴甲基)甲苯 反应生成5-甲基-1,3-二乙氰基苯
参考文献:(Substituted Aralkyl) Heterocyclic Compounds
标题:(Substituted Aralkyl) Heterocyclic Compounds
摘要:一种式子i的(A-取代-芳基)杂环化合物,其中r1是一个叠氮基,氨基甲酰基,氰基,甲酰基,羟基或硝基基团,1-6C 1-羟基烷基,烷氧基,烷基氨甲酰基,烷基硫醇基,烷基亚磺酰基或烷基磺酰基基团,2-氰基乙基基团,可选地带有1-4个1-6C烷基取代基,或2-6C脂肪酰基,卤代脂肪酰基,脂肪酰氧基,脂肪酰氨基,二烷基氨基甲酰基或烷氧羰基基团;R2和r3可以相同也可以不同,分别是氢原子,1-6C烷基,二氘烷基或卤代烷基基团,或苯基或苯基(1-6C烷基)基团,在其中苯基可以可选地带有一个或多个取代基;或r2和r3与它们附着的碳原子一起可以形成一个3-到6-成员的环;或r1 R2 R3 C-是一个1,1-二氰基乙基基团或三氟甲磺酰基基团;R4是氢或卤素原子,氰基或硝基基团或1-6C烷基或卤代烷基基团;R5具有上述定义的r1 R2 R3 C基团的任何值,但不一定与r1 R2 R3 C相同,或具有上述定义的r4的任何值,但不一定与r4相同,或是一个氨甲酰基,1-吡咯啉基甲酰基,哌啶基甲酰基,吗啉基甲酰基或硝基基团,1-6C烷氧基或卤代烷氧基基团或2-6C脂肪酰基或烷氧羰基基团;A是一个亚甲基或乙烯基基团,可选地带有一个或多个取代基,所选取代基包括氘和卤素原子,氨基甲酰基,氰基和羟基基团,1-6C烷基和烷氧基团,以及2-6C脂肪酰氧基基团,但当a通过其氮原子与r6连接时,它不得在与该氮原子相邻的碳原子上带有羟基,烷氧基或脂肪酰氧基取代基;R6是1H-1,2,4-三唑-1-基,4H-1,2,4-三唑-4-基,1H-咪唑-1-基,5-氰基-1H-咪唑-1-基,3-吡啶基或5-嘧啶基基团,或1H-咪唑-1-基,其在5-位置带有一个1-6C烷基取代基,该1-6C烷基本身可选地被一个或多个氨基甲酰基,氰基,羟基或2-6C烷氧羰基基团取代;并且当r2,R3,R4和r5为氢时,A是一个亚甲基基团,R6是3-吡啶基基团,R1不是氰基,羟基或羟甲基基团,当r1是羟基基团时,R3,R4和r5为氢,A是亚甲基基团,R6是3-吡啶基,R2不是甲基或2-氯-1-甲基乙基基团,当r1是甲氧羰基基团时,R2,R3,R4和r5为氢,A是亚甲基基团,R1不是1H-咪唑-1-基;以及其药学上可接受的酸盐.

专利信息

专利号:US-2006035950-A1
优先权日:2004-08-09
标 题:Novel processes for preparing substantially pure anastrozole
发明人：ALNABARI MOHAMMED; FREGER BORIS; ARAD ODED; ZELIKOVITCH LIOR; SERYI YANA; DANON EDNA; DAVIDI GUY; KASPI JOSEPH
权利人:ALNABARI MOHAMMED; FREGER BORIS; ARAD ODED; ZELIKOVITCH LIOR; SERYI YANA; DANON EDNA; DAVIDI GUY; KASPI JOSEPH
摘要:The present invention provides novel processes for purifying anastrozole, devoid of using liquid chromatography. The purification processes are via the isolated anastrozole salt forms, either by crystallization or by selective acidic extractions, and optionally in both cases, converting the purified anastrozole salt to anastrozole base. Also provided is an improved process for the synthesis of anastrozole, which is obtained by alkylating the isolated and purified starting material 3,5-bis(2-cyanoprop-2-yl)benzylbromide, the process being devoid of using toxic, hazardous and environmental unfriendly solvents and reagents.