CAS: 120511-92-4; 2,2'-(5-((4H-1,2,4-Triazol-4-yl)Methyl)-1,3-Phenylene)Bis(2-Methylpropanenitrile)

该化合物是一种与Aastrozole 结构相关的血清芳香酶抑制剂,其结构上与Aastrozole有关,旨在有选择地抑制对雌激素生物合成负责的芳香酶酶,其主要优点包括芳香酶具有高度特性,尽可能减少目标外效应,与早期抑制剂相比,代谢稳定性得到改善.复合物显示出对雌激素生产的强烈抑制,使其与对荷尔蒙依赖性条件下的研究相关.其优化的药用植物基因特征允许持续的生物利用率和长期活动.Isoanastrozole 的抗血压性骨骼可能有助于减少与细胞色素P450酶的相互作用,从而可能降低药物相互作用的风险.这些特性使该物质成为在临床前和临床环境中研究雌激素调节的一种宝贵工具.

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112809-27-5 1249332-95-3 36175-43-6

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1,2,4-Triazole α,α,α',α'-tetramethyl-5-chloromethyl-1,3-benzene diacetonitrile sodium triazole 2-[3-bromomethyl-5-(cyanodimethylmethyl)phenyl]-2-methylpropanenitrile

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    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.

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    主要参考文献

    1. Behan LA, Amir E, Casper RF. Aromatase inhibitors for prevention of breast cancer in postmenopausal women: a narrative review. Menopause. 2015;22(3):342-350. doi:10.1097/GME.0000000000000426 2. Howell A. New developments in the treatment of postmenopausal breast cancer. Trends Endocrinol Metab. 2005;16(9):420-428. doi:10.1016/j.tem.2005.09.003 3. Markopoulos CJ. Minimizing early relapse and maximizing treatment outcomes in hormone-sensitive postmenopausal breast cancer: efficacy review of AI trials. Cancer Metastasis Rev. 2010;29(4):581-594. doi:10.1007/s10555-010-9248-x
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