反应详情

Boc-D-Tic-OH (4.50 g, 16 mmol), methoxymethylamine hydrochloride (1.56 g, 16 mmol), HOBT (2.43 g, 18 mmol), EDC (3.45 g, 18 mmol), DMAP (200 mg, 1.6 mmol), DIPEA (4.2 ml) and THF (150 ml) are combined, and the resulting mixture is stirred for about 18 hours at r.t. The mixture is stripped to dryness, and the resulting residue is taken up in ethyl acetate and then washed with aqueous HCl (1N), aqueous sodium bicarbonate and brine, which is then dried over sodium sulfate. The solvent is removed and the residue is chromatographed on normal phase (ethylacetate/hexanes 1:1) to give about 3.89 g of Boc-D-Tic-NMeOMe (Weinreb amide).

1. washwashed with aqueous HCl (1N), aqueous sodium bicarbonate and brine, which
2. dry with materialis then dried over sodium sulfate
3. customThe solvent is removed
4. customthe residue is chromatographed on normal phase (ethylacetate/hexanes 1:1)