On April 4, 2013, Cho, Young Shin; Levell, Julian Roy; Toure, Bakary-Barry; Yang, Fan; Caferro, Thomas; Lei, Huangshu; Lenoir, Francois; Liu, Gang; Palermo, Mark G.; Shultz, Michael David; Smith, Troy; Costales, Abran Q.; Pfister, Keith Bruce; Sendzik, Martin; Shafer, Cynthia; Sutton, James; Zhao, Qian published a patent.Synthetic Route of 168297-86-7 The title of the patent was 3-Pyrimidin-4-yl-oxazolidin-2-ones as inhibitors of mutant IDH and their preparation. And the patent contained the following:
The invention is directed to a compound of formula I or a pharmaceutically acceptable salt thereof, and to the use of such compounds in the inhibition of mutant IDH proteins having a neomorphic activity. Compounds of formula I wherein R1 and R2 are independently H, D, halo, OH, etc.; R3a is H, D, C1-6 alkyl, Ph, and benzyl; R3b is H, D, and C1-6 alkyl; R4a is H, C1-6 alkyl, (un)substituted Ph, (un)substituted benzyl, etc.; R4b is H, D, and C1-3 alkyl; R3aR3b or R4aR4b can be taken together to form (un)substituted 3- to 7-membered cycloalkyl and (un)substituted 4- to 7-membered heterocyclyl; R5a is H and D; R5b is H, D, Me, Et, CF3, CD3, etc.; R6 is (un)substituted C1-6 alkyl, (un)substituted heteroaryl, (un)substituted aryl, etc.; R5bR6 can be taken together to form (un)substituted C3-7 cycloalkyl, (un)substituted bicycloalkyl; and pharmaceutically acceptable salts thereof, are claimed. Example compound II was prepared by amination of (S)-3-(2-chloropyrimidin-4-yl)-5,5-dimethyl-4-phenyloxazolidin-2-one with (S)-(-)-1-phenylethanamine. All the invention compounds were evaluated for their IDH inhibitory activity. From the assay, it was determined that compound II exhibited IC50 values in the range of 0.084 μM to 0.236 μM. The experimental process involved the reaction of (S)-4-Isopropyl-5,5-dimethyloxazolidin-2-one(cas: 168297-86-7).Synthetic Route of 168297-86-7
The Article related to pyrimidinyloxazolidinone preparation mutant idh inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Synthetic Route of 168297-86-7
Referemce:
Oxazolidine – Wikipedia,
Oxazolidine | C3H7NO – PubChem