Preparation of (−)-Nutlin-3 using enantioselective organocatalysis at decagram scale

…, AE Vilgelm, A Richmond, JN Johnston

文献索引：Davis, Tyler A.; Vilgelm, Anna E.; Richmond, Ann; Johnston, Jeffrey N. Journal of Organic Chemistry, 2013 , vol. 78, # 21 p. 10605 - 10616

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被引用次数: 25

摘要

Chiral nonracemic cis-4, 5-bis (aryl) imidazolines have emerged as a powerful platform for the development of cancer chemotherapeutics, stimulated by the Hoffmann-La Roche discovery that Nutlin-3 can restore apoptosis in cells with wild-type p53. The lack of efficient methods for the enantioselective synthesis of cis-imidazolines, however, has limited their more general use. Our disclosure of the first enantioselective synthesis of (−)-Nutlin-3 ...