反应详情

To an ice-cooled and stirred solution of 2-amino-3-benzoyl4,5,6,7-tetrahydrothieno[2,3-c]pyridine (0.775 mmol) in dry DMF (11 mL), was added BOC-Tyr-OH (0.08 mmol) and EDCl (0.08, 0.445 g) under an argon atmosphere. After stirring overnight, the mixture was evaporated under vacuum to give a solid residue, which was dissolved in a saturated sodium bicarbonate solution and is extracted with ethyl acetate (3×20 mL), then dried on magnesium sulfate. The organic layers were evaporated under vacuum to give a solid which is chromatographed on silica gel column eluting with ethyl acetate and petroleum ether to afford 2-amino-3-benzoyl-6-[2-t-butoxycarbonylamino-3-(4-hydroxyphenyl)-propion-yl]-4,5,6,7-tetrahydrothieno[2,3-c]pyridine a yellow solid.

1. customthe mixture was evaporated under vacuum
2. customto give a solid residue, which
3. extractionis extracted with ethyl acetate (3×20 mL)
4. customdried on magnesium sulfate
5. customThe organic layers were evaporated under vacuum
6. customto give a solid which
7. customis chromatographed on silica gel column
8. washeluting with ethyl acetate and petroleum ether