抗癌药来曲唑的合成研究
Study on the Synthesis of Letrozole
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摘要: 芳香化酶能选择性地催化雌激素生物合成的最后一步,对它的抑制能在不影响其它甾体激素生物合成的情况下,专一性地降低雌激素水平,是一类疗效很好的抗乳腺癌药物。来曲唑(Letrozole,1)是一种非甾体高效选择性芳香化酶抑制剂,1996年首次在英国上市,1997年获得FDA批准,临床上用于治疗妇女晚期乳腺癌。在体内来曲唑降低血浆雌激素水平的能力是法屈唑的8倍,Abstract: AIM:To develop a method for preparation of letrozole . METHOD: Aniline is used as starting material to prepare letrozole by reactions of condensation, diazotization,bromination and condensation. RESULT: The structure of synthesized letrozole is confirmed