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来那度胺合成路线图解

Graphical synthetic routes to lenalidomide
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摘要 来那度胺(1enalidomide,1),化学名为3-(4-氨基-1,3-二氢-1-氧代-2H-异吲哚-2-基)-2,6-哌啶二酮,CAS登记号:191732—72-6,商品名:Rev—limid,是由美国Celgene公司研发的新型免疫调节剂。于2006年1月在美国批准上市,临床主要用于治疗5号染色体长臂(5q)缺失的骨髓增生异常综合征亚型及多发性骨髓瘤。来那度胺是沙利度胺的衍生物,与沙利度胺相比,其药效约强一百倍,且目前没有发现致畸变作用。本品可以激活T细胞,进而产生白细胞介素2(IL乏),增强自然杀伤细胞(NK细胞)的免疫活性,从而发挥其免疫调节作用。本文综述了来那度胺的合成方法,合成路线见图l。 Lenalidomide is a new immune modulator. Lenalidomide was used for the treatment of 5q deletion myelodysplastic syndrome and multiple myeloma. It was discovered by Celgene in America. Lenalidomide has been approved for marketing in America in 2006.There are many ways to total synthesis of this compound. We listed these five methods so as to make contribution to further application and research.
出处 《中国药物化学杂志》 CAS CSCD 2014年第4期327-329,4,共3页 Chinese Journal of Medicinal Chemistry
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