反应详情

In the same way as described for Compound 154, step 1 using 1-iodo-4-nitrobenzene (0.498 g, 2.0 mmol), 1-dimethylamino-2-propyne (0.216 mL, 2.00 mmol), L-proline (46.1 mg, 0.40 mmol), Na2CO3 (42.4 mg, 0.40), NaN3 (0.156 g, 2.40 mmol), (+)-sodium-L-ascorbate (39.7 mg, 0.20 mmol), copper(II) sulphate pentahydrate (16.0 mg, 0.10 mmol) in 9:1 DMSO-water (4 mL). The residue is purified on Isolute FlashSilicaII cartridge eluting with 97:3 DCM:NH3 (7M in MeOH), to afford the title compound as a brown solid (0.179 g, 36%).

1. customThe residue is purified on Isolute FlashSilicaII cartridge
2. washeluting with 97:3 DCM