Discovery of 5,6,7,8-tetrahydropyrido[3,4-d]pyrimidine inhibitors of Erk2 was written by Blake, James F.;Gaudino, John J.;De Meese, Jason;Mohr, Peter;Chicarelli, Mark;Tian, Hongqi;Garrey, Rustam;Thomas, Allen;Siedem, Christopher S.;Welch, Michael B.;Kolakowski, Gabrielle;Kaus, Robert;Burkard, Michael;Martinson, Matthew;Chen, Huifen;Dean, Brian;Dudley, Danette A.;Gould, Stephen E.;Pacheco, Patricia;Shahidi-Latham, Sheerin;Wang, Weiru;West, Kristina;Yin, Jianping;Moffat, John;Schwarz, Jacob B.. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2014.Synthetic Route of C8H9ClFNO The following contents are mentioned in the article:
The discovery and optimization of a series of tetrahydropyridopyrimidine based extracellular signal-regulated kinase (Erks) inhibitors discovered via HTS and structure based drug design is reported. The compounds demonstrate potent and selective inhibition of Erk2 and knockdown of phospho-RSK levels in HepG2 cells and tumor xenografts. Proliferation of HCT116 (K-RasG12D) and A375 (BRafV600E) cell lines was inhibited by compound (I) with EC50s of 0.74 and 0.39 μM, resp. Pharmacokinetic parameters of I are given. This study involved multiple reactions and reactants, such as (S)-2-Amino-2-(3-chloro-4-fluorophenyl)ethanol (cas: 496856-52-1Synthetic Route of C8H9ClFNO).
(S)-2-Amino-2-(3-chloro-4-fluorophenyl)ethanol (cas: 496856-52-1) belongs to alcohols. Because alcohols are easily synthesized and easily transformed into other compounds, they serve as important intermediates in organic synthesis. Tertiary alcohols cannot be oxidized at all without breaking carbon-carbon bonds, whereas primary alcohols can be oxidized to aldehydes or further oxidized to carboxylic acids.Synthetic Route of C8H9ClFNO
Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts