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- W3197858900 abstract "KGP94 is a potent, selective, and competitive inhibitor of the lysosomal endopeptidase enzyme (Cathepsin L) currently in preclinical trials for the treatment of metastatic cancer, which is a leading cause of cancer-associated death. Herein, we report two new synthetic routes for synthesizing the target compound through four consecutive steps, using a Weinreb amide approach starting from a common 3-bromobenzoyl chloride. A key step in the approach is a coupling reaction of a readily available Grignard reagent with amide 4 to produce 6, a previously unreported coupling pattern. These new strategies offer an efficient and alternative approach to synthesis of target compound with an excellent overall yield." @default.
- W3197858900 created "2021-09-13" @default.
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- W3197858900 date "2021-11-01" @default.
- W3197858900 modified "2023-09-23" @default.
- W3197858900 title "An efficient and concise synthesis of a selective small molecule non-peptide inhibitor of cathepsin L: KGP94" @default.
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- W3197858900 doi "https://doi.org/10.1016/j.bioorg.2021.105317" @default.
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