Albrecht, Brian K. et al. published their patent in 2013 |CAS: 65417-22-3

The Article related to heteroaryl amide preparation methyl modifying enzyme modulator antitumor, mutant ezh2 protein cancer treatment heteroaryl amide preparation, Heterocyclic Compounds (One Hetero Atom): Pyridines and other aspects.Synthetic Route of 65417-22-3

On August 15, 2013, Albrecht, Brian K.; Audia, James Edmund; Cook, Andrew S.; Dakin, Les A.; Duplessis, Martin; Gehling, Victor S.; Harmange, Jean-Christophe; Naveschuk, Christopher G.; Vaswani, Rishi G. published a patent.Synthetic Route of 65417-22-3 The title of the patent was Preparation of heteroaryl amides as modulators of methyl modifying enzymes. And the patent contained the following:

The title compounds I [Z = CR2 or N; X1, X2 = N, CR3; X3 = N, CR6; no more than one of X1-X3 = N; R1, R2 = H, halo, OH, CN, etc.; or R1 and R2 are taken together with atoms to which they are bound to form (hetero)aryl, heterocyclyl, cycloalkyl; R3, R6 = H, halo, CN, etc.; or two R3 are taken together with atoms to which they are bound to form (hetero)aryl, heterocyclyl, cycloalkyl; R = (hetero)aryl, heterocyclyl, cycloalkyl, etc.], useful as agents for modulating Me modifying enzymes, were prepared Thus, reacting 3-(aminomethyl)-4,6-dimethylpyridin-2(1H)-one with 5-methyl-1-phenyl-1H-pyrazole-4-carboxylic acid afforded 26% II. Exemplified compounds I were tested against EZH2 and Y641N EZH2 mutant enzymes (data given for representative compounds I). Pharmaceutical composition comprising I is disclosed. The experimental process involved the reaction of Methyl 2-methyl-1H-indole-3-carboxylate(cas: 65417-22-3).Synthetic Route of 65417-22-3

The Article related to heteroaryl amide preparation methyl modifying enzyme modulator antitumor, mutant ezh2 protein cancer treatment heteroaryl amide preparation, Heterocyclic Compounds (One Hetero Atom): Pyridines and other aspects.Synthetic Route of 65417-22-3

Referemce:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles