Convergent, kilogram scale synthesis of an Akt kinase inhibitor

…, RS Hoerrner, M Weisel, J Arredondo…

文献索引：Grongsaard, Pintipa; Bulger, Paul G.; Wallace, Debra J.; Tan, Lushi; Chen, Qinghao; Dolman, Sarah J.; Nyrop, Jason; Hoerrner, R. Scott; Weisel, Mark; Arredondo, Juan; Itoh, Takahiro; Xie, Chengfu; Wen, Xianghui; Zhao, Dalian; Muzzio, Daniel J.; Bassan, Ephraim M.; Shultz, C. Scott Organic Process Research and Development, 2012 , vol. 16, # 5 p. 1069 - 1081

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被引用次数: 18

摘要

The development of a convergent, chromatography-free synthesis of an allosteric Akt kinase inhibitor is described. The route comprised 17 total steps and was used to produce kilogram quantities of the target molecule. A key early transformation, for which both batch and flow protocols were developed, was formylation of a dianion derived by deprotonation and subsequent lithium-halogen exchange from a 2-bromo-3-aminopyridine precursor. ...