On October 24, 2019, Lauffer, David J.; Bemis, Guy; Boyd, Michael; Deininger, David; Deng, Hongbo; Dorsch, Warren; Gu, Wenxin; Hoover, Russell R.; Johnson, Jr., Mac Arthur; Ledeboer, Mark Willem; Ledford, Brian; Maltais, Francois; Penney, Marina; Takemoto, Darin; Waal, Nathan D.; Weng, Tiansheng published a patent.Application of 386704-04-7 The title of the patent was Preparation of pteridinone compounds for the treatment of cellular proliferative disorders. And the patent contained the following:
The invention provides compounds of formula I, or pharmaceutically acceptable salts thereof, pharmaceutical compositions thereof, and methods of use thereof for treating cellular proliferative disorders (e.g., cancer). Compounds of formula I wherein A is (un)saturated 3- to 8-membered carbocyclic ring, indanyl, Ph, (un)saturated 4- to 8-membered monocyclic heterocyclic ring; L is a bond, (un)branched C1-6 hydrocarbyl and (un)branched C1-6 heterohydrocarbyl; R1 is H, (un)substituted C1-4 aliphatic, R’, etc.; R2 and R2′ are independently H, R’, (un)substituted C1-4 aliphatic, etc.; R3 is H, R’, and (un)substituted C1-6 aliphatic; R4 is H, R’, CH2OH, etc.; R5 is H, acyl, CO2H and derivatives, etc.;each R6 is independently halo, CN, NO2, acyl, etc.; R’ is C1-4 deuterioaliph.; X is N and CH; n is 0, 1, 2, 3, 4 and 5; and pharmaceutically acceptable salts thereof, are claimed. Example compound II was prepared by a general procedure (procedure given). The invention compounds were evaluated for their PLK1 inhibitory activity. From the assay, it was determined that compound II exhibited IC50 value of < 0.3 μM. The experimental process involved the reaction of (6-(Trifluoromethyl)pyridin-3-yl)methanol(cas: 386704-04-7).Application of 386704-04-7
The Article related to pteridinone preparation treatment cellular proliferative disorder, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Application of 386704-04-7
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