反应详情

Boc-D-Tic-OH (14.9 g, 53.7 mmol), methoxymethylamine hydrochloride (5.24 g, 53.7 mmol), EDC (11.3 g, 59.1 mmol); HOBT (7.98 g, 59.1 mmol), DIPEA (9.83 ml, 59.1 mmol) and THF (500 ml) are combined, and the resulting mixture is stirred for about 18 hours at r.t. under nitrogen. The mixture is stripped to dryness, and the residue is taken up in ethyl acetate. The resulting mixture is washed with 1M HCl, saturated NaHCO3 and brine, and then dried. Solvent is removed and the residue is chromatographed on normal phase using 1:1 ethylacetate/hexane to give about 12.3 g of Boc-D-Tic-NMeOMe (Weinreb amide).

1. washThe resulting mixture is washed with 1M HCl, saturated NaHCO3 and brine
2. customdried
3. customSolvent is removed
4. customthe residue is chromatographed on normal phase