反应详情

4-(4-Carboxy-thiophen-2-yl)-3,6-dihydro-2H-pyridine-1-carboxylic acid tert-butyl ester (0.1 g, 0.35 mmol) was dissolved in DMF (2 mL) and triethylamine (1.0 mmol). Homopiperidine (1.4 mmol) was added with HATU (0.35 mmol) and the mixture stirred for 2 hours. The mixture was diluted with DCM (20 mL) and washed with water. The organic solution was separated, dried with anhydrous magnesium sulphate, filtered and evaporated. The residue was then purified by HPLC, eluting with 10%-98% acetonitrile in water (0.1% formic acid) over 30 minutes. The fractions containing the desired product were concentrated under vacuum to give the title compound (0.095 g). LCMS m/z 391.56 [M+H]+ RT=4.09min (Analytical Method 4).

1. washwashed with water
2. customThe organic solution was separated
3. dry with materialdried with anhydrous magnesium sulphate
4. filtrationfiltered
5. customevaporated
6. customThe residue was then purified by HPLC
7. washeluting with 10%-98% acetonitrile in water (0.1% formic acid) over 30 minutes
8. additionThe fractions containing the desired product
9. concentrationwere concentrated under vacuum