阿那曲唑及其衍生物的合成

阿那曲唑及其衍生物的合成 01-I-002 阿那曲唑及其衍生物的合成 *王立升～李钰 广西大学化学化工学院，530004，南宁 E-mail: lswang@gxu.edu.cn 实验合成了阿那曲唑，并对其合成工艺进行了改进。为了寻找抗乳腺癌作用强，毒性小的芳香 酶抑制剂，以阿那曲唑为先导化合物，保留其对称结构部分，对其进行结构修饰，设计并合成了十 1三个未见文献报道的衍生物，并经IR、MS和H-NMR确证其化学结构。药理活性实验正在进行中。 NNNNNNNNNCH3R=NNNCNN O CHRO3NONNNNNOOCH3CH3O ONNNNCHO3CNNNNONHNNHHNOCNHCN25 Fig.1 Structures of anastrozole and its derivatives 关键词:芳香酶抑制剂;阿那曲唑;结构修饰。 参考文献: [1] F. Boccardo, A. Rubagotti, M. Puntoni, et al. Switching to Anastrozole Versus Continued Tamoxifen Treatment of Early Breast Cancer: Preliminary Results of the Italian Tamoxifen Anastrozole Trial[J]. Journal of Clinical Oncology, Vol 23, No 22 (August 1), 2005, 23(22), 5138-5147 . [2] J. Correia, M. E. F. Braibante, L. Cotarca, et al. Studies Towards Streptonigrinoids: Formal Synthesis of Lavendamycin Methyl Ester[J]. J. synthesis. 1994, 1127. Synthesis of Anastrozole and Its Derivatives *Lisheng Wang, Yu Li College of Chemistry and Chemical Engineering, Guangxi University, 530004, Nanning Anastrozole was synthesized using an improved method. Based on anastrozole as the leading compound, we designed and synthesized a series of unreported anastrozole derivatives, which structures were 1confirmed by IR, MS and H-NMR. 01-012