A practical synthesis of 5-(chloromethyl)furo[2,3-<i>b</i>]pyridine, a key intermediate for the HIV protease inhibitor, L-754,394
作者:M. Bhupathy、David A. Conlon、Kenneth M. Wells、John R. Nelson、Paul J. Reider、Kai Rossen、Jess W. Sager、R. P. Volante、Bruce D. Dorsey、Jacob M. Hoffman、Sally A. Joseph、Stacey L. Mcdaniel
DOI:10.1002/jhet.5570320431
日期:1995.7
A practical synthesis of 5-(chloromethyl)furo[2,3-b]pyridine (10), the side chain used to incorporate a key pharmacophore of the HIV protease inhibitor, L-754,394, is described. The synthesis was accomplished in ten steps and in 15% overall yield from commercially available methyl 2-furoate.
描述了一种实用的合成方法,即5-(氯甲基)呋喃并[2,3- b ]吡啶(10),侧链用于掺入HIV蛋白酶抑制剂的关键药效基团L-754,394。所述合成以十个步骤完成,并且由市售的2-糠酸甲酯的总产率为15%。