750633-66-0Relevant articles and documents
An efficient and concise synthesis of a selective small molecule non-peptide inhibitor of cathepsin L: KGP94
Munikishore, Rachakunta,Wang, Liang-Liang,Zhang, Shuqun,Zhao, Qin-Shi,Zuo, Zhili
, (2021/09/06)
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.
Palladium-catalyzed C-H activation/intramolecular amination reaction: A new route to 3-aryl/alkylindazoles
Inamoto, Kiyofumi,Saito, Tadataka,Katsuno, Mika,Sakamoto, Takao,Hiroya, Kou
, p. 2931 - 2934 (2008/02/07)
A method for the catalytic C-H activation of hydrazone compounds followed by intramolecular amination is described. It requires the use of a catalytic amount of Pd(OAc)2 in the presence of Cu(OAc)2 and AgOCOCF3, which effi