反应详情

A mixture of N-{4-methyl-5-[2-(1-methyl-cyclopropyl)-pyridin-4-yl]-thiazol-2-yl}-acetamide (Step 401.3) (565 mg, 7 mmol), a 6N aqueous solution of HCl (3 mL) and EtOH (15 mL) is stirred for 3.5 h at 85° C., allowed to cool, quenched by addition of a saturated solution of NaHCO3 and extracted with DCM. The organic phase is washed with a saturated solution of NaHCO3, dried (Na2SO4), filtered and concentrated. The residue is purified by silica gel column chromatography (DCM/MeOH, 1:0→98:2) to afford 366 mg of the title compound as a yellow solid: ESI-MS: 246.1 [M+H]+; TLC: Rf=0.40 (DCM/MeOH, 9:1).

1. temperatureto cool
2. customquenched by addition of a saturated solution of NaHCO3
3. extractionextracted with DCM
4. washThe organic phase is washed with a saturated solution of NaHCO3
5. dry with materialdried (Na2SO4)
6. filtrationfiltered
7. concentrationconcentrated
8. customThe residue is purified by silica gel column chromatography (DCM/MeOH, 1:0→98:2)