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公开(公告)号:US09296780B2
公开(公告)日:2016-03-29
申请号:US14367886
申请日:2012-12-19
CPC分类号: C07J75/00 , C07J1/0011 , C07J1/0059 , C07J1/0081 , C07J1/0096 , C07J7/00 , C07J7/0055 , C07J7/0075 , C07J7/009 , C07J31/006 , C07J51/00
摘要: A process ethynylates 16-methylene-17-keto steroids to the corresponding 16-methylene-17α-ethynyl-17β-hydroxy steroids by treatment with silyl-protected lithium acetylides followed by further desilylation. The resulting products are useful intermediates in the preparation of several pharmaceutically active agents, such as e.g. Nestorone® or melengestrol acetate.
摘要翻译: 通过用甲硅烷基保护的乙炔化锂处理,然后进一步脱甲硅烷,将16-亚甲基-17-酮类固醇乙炔化为相应的16-亚甲基-17α-乙炔基-17β-羟基类固醇。 所得产物是制备几种药物活性剂的有用的中间体,例如 Nestorone®或醋酸美伦他林。