【药物名称】K-777, CRA-3316, APC-3316, K-11777
化学结构式(Chemical Structure):
参考文献No.53983
标题:Irreversible cysteine protease inhibitors containing vinyl groups conjugated to electron withdrawing groups
作者:Palmer, J.T.; Rasnick, D.; Klaus, J.L. (Celera Genomics)
来源:US 6287840
合成路线图解说明:

Phosphonylation of the lithium anion of phenyl methyl sulfone (I) with diethyl chlorophosphate afforded the sulfonyl phosphonate (II). This was condensed with N-Boc-L-homophenylalaninal (III) under Wadsworth-Emmons conditions to furnish the vinyl sulfone (IV). After acidic Boc group cleavage, the resultant amine (V) was coupled with the N-carbamoyl phenylalanine (VI), via the corresponding mixed anhydride with isobutyl chloroformate, to afford the target amide.

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