With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.7651-81-2,Isoquinolin-3(2H)-one,as a common compound, the synthetic route is as follows.
tert-butyl 3-(hydroxymethyl)-2-azabicyclo[3.1.1]heptane-2-carboxylate (p14, 100 mg, 0.44 mmol) was dissolved in THF (7 mL). PP (174 mg, 0.66 mmol) was added, followed by 3-hydroxyisoquinoline (96 mg, 0.66 mmol). The mixture was stirred at RT for 15′, then cooled to 0 C. Di-tert-butyl azodicarboxylate (152 mg, 0.66 mmol) was added portionwise and, after 10′, the ice bath was removed, allowing the mixture to stir at RT for 1 .5h. The mixture was concentrated under vacuum to obtain a crude that was combined with crude from a similar preparation. Combined crude material was purified by FC on silica gel (eluent from Cy to EtOAc 20%) to afford tert-butyl 3-[(isoquinolin-3- yloxy)methyl]-2-azabicyclo[3.1.1 ]heptane-2-carboxylate (p16, 72 mg, 30% recovery on combined batches) as colourless oil. MS (mlz): 355.3 [MH]+., 7651-81-2
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Reference£º
Patent; CHRONOS THERAPEUTICS LIMITED; MICHELI, Fabrizio; BERTANI, Barbara; GIBSON, Karl Richard; DI FABIO, Romano; RAVEGLIA, Luca; ZANALETTI, Riccardo; CREMONESI, Susanna; POZZAN, Alfonso; SEMERARO, Teresa; TARSI, Luca; LUKER, Timothy Jon; (275 pag.)WO2019/43407; (2019); A1;,
Isoquinoline – Wikipedia
Isoquinoline | C9H7N – PubChem