Electric Literature of 768-70-7,Some common heterocyclic compound, 768-70-7, name is 3-Ethynylanisole, molecular formula is C9H8O, traditional synthetic route has been very mature, but the traditional synthetic route has various shortcomings, such as complicated route, low yield, poor purity, etc, below Introduce a new synthetic route.
A solution consisting of 2-(3-iodo-4-methoxybenzoyl)isoindoline (50 mg, 0.132 mmol), 3- ethynylanisole (52 mg, 0.396 mmol), CuI (5 mg, 0.026 mmol), Pd(PPh3J2CI2 (18 mg, 0.026) and TEA (0.055 ml_, 0.396 mmol) in 7.5 ml. of toluene was stirred under nitrogen overnight in a 40 ml_ vial at 1000C. Upon cooling to rt, the crude mixture was filtered through a plug of silica gel and washed through with EtOAc. The solvents were then removed under reduced pressure and the residue was purified by flash chromatography on silica gel (20:1 CH2CI2/Me0H) to afford 35 mg (69%) of the title compound as an off-white solid. 1H NMR (400 MHz, CDCI3): consistent; MS (ES+) mlz 384.1 (M+H).
The synthetic route of 768-70-7 has been constantly updated, and we look forward to future research findings.
Reference:
Patent; WYETH LLC; LI, David, Zenan; O’NEIL, Steven, Victor; SPRINGER, Dane, Mark; ZEGARELLI, Benjamin, Miller; WO2010/124047; (2010); A1;,
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