Molbank
(Apr 2020)
Improved Synthesis and Determination of the Biologically Active Diastereomer of YK11
Yuichiro Kanno,
Taichi Kusakabe,
Nao Saito,
Shoko Kikkawa,
Keisuke Takahashi,
Isao Azumaya,
Kiyomitsu Nemoto,
Keisuke Kato
Affiliations
Yuichiro Kanno
Faculty of Pharmaceutical Sciences, Toho University, 2-2-1 Miyama, Funabashi, Chiba 274-8510, Japan
Taichi Kusakabe
Faculty of Pharmaceutical Sciences, Toho University, 2-2-1 Miyama, Funabashi, Chiba 274-8510, Japan
Nao Saito
Faculty of Pharmaceutical Sciences, Toho University, 2-2-1 Miyama, Funabashi, Chiba 274-8510, Japan
Shoko Kikkawa
Faculty of Pharmaceutical Sciences, Toho University, 2-2-1 Miyama, Funabashi, Chiba 274-8510, Japan
Keisuke Takahashi
Faculty of Pharmaceutical Sciences, Toho University, 2-2-1 Miyama, Funabashi, Chiba 274-8510, Japan
Isao Azumaya
Faculty of Pharmaceutical Sciences, Toho University, 2-2-1 Miyama, Funabashi, Chiba 274-8510, Japan
Kiyomitsu Nemoto
Faculty of Pharmaceutical Sciences, Toho University, 2-2-1 Miyama, Funabashi, Chiba 274-8510, Japan
Keisuke Kato
Faculty of Pharmaceutical Sciences, Toho University, 2-2-1 Miyama, Funabashi, Chiba 274-8510, Japan
DOI
https://doi.org/10.3390/M1125
Journal volume & issue
Vol. 2020,
no. 2
Abstract
Read online
The palladium catalyzed carbonylation of 1 using the chiral ligand L1 afforded 2 in a highly diastereoselective manner. The stereochemistry of the major diastereomer 2a was determined by X-ray crystallographic analysis. AR luciferase reporter assay studies suggested that 2a was the active constituent of YK11 (2).
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