4-Thiazolemethanol, 2-ethyl- synthesis

Yield:937663-77-9 65%

Reaction Conditions:

with methanol;sodium tetrahydridoborate at 20;

Steps:

XXX.1 Step 1 : (2-Ethylthiazol-4-yl)methanol

Step 1 : (2-Ethylthiazol-4-yl)methanol To a solution of ethyl 2-ethylthiazole-4-carboxylate (1 g, 5.4 mmol) in CH₃OH (20ml) was added NaBH₄ (2.04 g, 54 mmol) by portion. The resulting mixture was stirred at room temperature. After TLC analysis showed the starting material was disappeared. The solvent was removed in vacuo. The residue was dissolved in DCM (50 mL) and washed with H₂0. The organic layer was dried and concentrated to give (2-ethylthiazol-4-yl) methanol (0.5 g, 65%): 1H NMR (400 MHz, CD₃OD) δ 7.23-7.22 (m, 1H), 4.64 (m, 2H), 3.03-2.98 (m, 3H), 1.35 (t, J = 7.6 Hz, 2H).

References:

WO2013/149362,2013,A1 Location in patent:Page/Page column 52