CAS: 120511-84-4; 2,2'-(5-(Bromomethyl)-1,3-Phenylene)Bis(2-Methylpropanenitrile)

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CAS号120511-72-0 5,α,α,α',α'-五甲基... | CAS号120511-73-1 阿那曲唑 | CAS号120511-92-4 2,2'-(5-((4H-1,... | CAS号120511-72-0 5,α,α,α',α'-五甲基...

五甲基-1,3-二乙氰基苯置于sodium Bromate,Sodium Hydrogensulfite体系中,用 水,乙酸乙酯 用作溶剂,化学反应生成5-溴甲基-A,A,A',A'-四甲基-1,3-二乙氰基苯
参考文献:基于阿那曲唑模板的双重芳香酶硫酸酯酶抑制剂:合成,体外sar,分子模型和体内活性.
标题:基于阿那曲唑模板的双重芳香酶硫酸酯酶抑制剂:合成,体外sar,分子模型和体内活性.
摘要:描述了一系列新型双重芳香酶-硫酸酯酶抑制剂(dasis)的合成和生物学评估.假定双重抑制芳香酶和类固醇硫酸酯酶,两者都负责雌激素的生物合成,在治疗激素依赖性乳腺癌中将是有益的.这些化合物基于阿那曲唑芳香化酶抑制剂模板,该模板在维持血红素连接三唑部分对酶抑制至关重要的同时,经过修饰,使其包括苯酚氨基磺酸酯基序,即有效抑制不可逆类固醇硫酸酯酶的药效基团.通过选择性自由基溴化和取代反应以提供一系列抑制性芳香化酶药效基团,可以使合成路线适应阿那曲唑.将这些片段连接至氨基磺酸氨基酚酯部分,使用s(n)2,Heck和mitsunobu反应与酚类前体进行反应,从中通过氨磺酰化反应完成dasi.在体外,先导化合物11对芳香化酶(ic(50)3.5 Nm)具有很高的效力,与阿那曲唑(ic(50)1.5 Nm)相当,而对甾族硫酸酯酶的活性却中等.然而,在体内,11出人意料地表现出有效的双重抑制作用.将化合物1
Doi:10.1039/b707768H

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.

专利号:WO-2007002722-A2
优先权日:2005-06-27
标题 :Synthesis of anastrozole and purification of one of its intermediate