The asymmetric synthesis of a 1,3-diamine building block for the elaboration of Bcl-2 and Bcl-xL protein inhibitors is described through two key steps: (1) a highly diastereoselective aza-Reformatsky reaction, and (2) a chemoselective amination under Mitsunobu conditions. This synthetic sequence was also demonstrated to be successfully amenable to a large-scale synthesis.
S. Laclef, C. Taillier, C. Penloup, A. Viger, J. Brière, C. Hardouin and V. Levacher, RSC Adv., 2014, 4, 39817 DOI: 10.1039/C4RA07821G
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