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Beilstein J. Org. Chem. 2021, 17, 156–165, doi:10.3762/bjoc.17.16
Graphical Abstract
Figure 1: Retrosynthetic disconnection of our privileged kinase scaffold 1.
Scheme 1: Reagents and conditions: (a) MeOH, DIPEA, reflux, 70%; b) TBTU, DIPEA, DMF, rt, 91%.
Scheme 2: Proposed mechanistic explanation for the liberation of the Pd catalytic cycle after addition of sac...
Scheme 3: Formation of C2–OAt ether 15 using HATU. Reagents and condtions: (a) HATU, DIPEA, DCM, rt, 16 h, ((...
Scheme 4: Proposed mechanistic pathways for the transformation of Py–OAt ethers 17 to the pyridin-2H-one 1 mo...
Scheme 5: Failure to exploit logical convergent building block 26. Reagents and conditions: a) HATU, DIPEA, D...
Scheme 6: Library route to 32. Reagents and conditions: a) 4 M HClaq, reflux, 1 h, 81%; (b) EDCI, pyridine, P...