Supplementary Methods from AG-221, a First-in-Class Therapy Targeting Acute Myeloid Leukemia Harboring Oncogenic IDH2 Mutations
Year: 2023
Type: supplementary-materials
Abstract: AG-221 chemical identityHRMS (m/z): [M+H] + calculated for C19H17F6N7O, 474.14715; found, 474.14600. AG-221 sample purityHPLC Purity = 97.8%,(Xtimate C18, 150*3.0mm, 3 um) 5-95% acetonitrile/water (0.1% TFA) over 15 minutes. Synthetic protocol 2-Methyl-1-(4-(6-(trifluoromethyl)-pyridin-2-yl)-6-(2-(trifluoromethyl)-pyridin-4-ylamino)-1,3,5triazin-2-ylamino)propan-2-ol (AG-221)To a solution of 4-chloro-6-(6-(trifluoromethyl)pyridin-2-yl)-N-(2-(trifluoro-methyl)-pyridin-4-yl)-1,3,5-triazin-2-amine (201.2 g, 0.48 mmol) in tetrahydrofuran (2 l) at room temperature, 1amino-2-methylpropan-2-ol (51.3 g, 0.58 mol) and NaHCO3 (60.5 g, 0.72 mol) was added.The mixture was heated at reflux for 16-24 hours, then concentrated under reduced pressure and
Authors: Katharine Yen, Jeremy Travins, Fang Wang, Muriel D. David, Erin Artin, Kimberly Straley, Anil Padyana, Stefan Gross, Byron DeLaBarre, Erica Tobin, Yue Chen, Raj Nagaraja, Sung Choe, Lei Jin, Zenon Konteatis, Giovanni Cianchetta, Jeffrey O. Saunders, Francesco G. Salituro, Cyril Quivoron, Paule Opolon, Olivia Bawa, Véronique Saada, Angelo Paci, Sophie Broutin, Olivier A. Bernard, Stéphane de Botton, Benoît S. Marteyn, Monika Pilichowska, YingXia Xu, Cheng Fang, Fan Jiang, Wentao Wei, Shengfang Jin, Lee Silverman, Wei Liu, Hua Yang, Lenny Dang, Marion Dorsch, Virginie Penard-Lacronique, Scott A. Biller, Shin-San Michael Su
Language: English
Subfield: Hematology
Field: Medicine
Domain: Health Sciences
Open Access status: gold
OpenAlex ID: W4362531446