Ethanol → (3R,4S)-4-(3',4'-Dichlorobiphenyl-4-yloxy)-1-pyridin-3-yl-pentan-3-ol oxalic acid salt

참여 물질

반응 조건

반응 단계

Prepared according to the method described in Example 12b) from 3,4-dichloro-iodobenzene (0.273 g), ethanol (2 ml), toluene (5 ml), 2M aqueous sodium carbonate (0.5 ml), (1S,2R)-4-[2-(tert-butyldimethylsilanyloxy)-1-methyl-4-pyridin-3-ylbutoxy]benzeneboronic acid (0.2 g, Example 11)), and tetrakis(triphenylphosphine)palladium (0) (0.025 g) with heating at 120° C. for 4 hours. After work-up, the residue was purified by normal-phase HPLC eluting a gradient of 0-25% ethanol in dichloromethane to give the title compound which was converted to the oxalic acid salt by treatment with a saturated ethereal solution of oxalic acid to give the title compound as a solid (0.229 g).

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