On September 8, 2017, Al-Awar, Rima; Zepeda-Velazquez, Carlos Armando; Poda, Gennady; Isaac, Methvin; Uehling, David; Wilson, Brian; Joseph, Babu; Liu, Yong; Subramanian, Pandiaraju; Mamai, Ahmed; Prakesch, Michael; Stille, Julia Kathleen published a patent.Quality Control of 4-(2-Bromopyrimidin-4-yl)morpholine The title of the patent was Preparation of N-aryl heteroarylcarboxamides and arylcarboxamides as inhibitors of WDR5 protein-protein binding. And the patent contained the following:
The application is directed to compounds of formula I and their uses, for example as medicaments for the treatment of diseases, disorders or conditions mediated or treatable by inhibition of binding between WDR5 protein and its binding partners. Compounds of formula I wherein R1 is (un)substituted heterocycloalkyl; R2 is (un)substituted C6-10 aryl and (un)substituted heteroaryl; R3 is (un)substituted C6-10 aryl, (un)substituted heteroaryl and (un)substituted heterocycloalkyl; X1 and X2 are independently CR17 and N; R17 is H, F, C1-6 alkyl and C1-6 fluoroalkyl; A is F, (fluoro)alkyl and (fluoro)alkylene; and pharmaceutically acceptable salts and solvates thereof, are claimed. Example compound II was prepared by multistep procedure (procedure given). The invention compounds were evaluated for their WDR5 protein binding affinity. From the assay, it was determined that compound II exhibited KD value of 0.084 μM. The experimental process involved the reaction of 4-(2-Bromopyrimidin-4-yl)morpholine(cas: 1209459-32-4).Quality Control of 4-(2-Bromopyrimidin-4-yl)morpholine
The Article related to aryl heteroarylcarboxamide arylcarboxamide preparation wdr5 protein binding inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Quality Control of 4-(2-Bromopyrimidin-4-yl)morpholine
Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia