反应详情

To a solution of 5-(3-benzyloxycarbonylamino-prop-1-ynyl)-thiophene-2-carboxylic acid tert-butyl ester (1.0 g, 2.69 mmol) in 15 mL MeOH and 2.69 mL 1 N HCl (aq) was added Pd(OH)2 (1 g). The mixture was shaken in a Parr shaker under 45 psi H2 for 16 h. The catalyst was removed by filtration through Celite and additional Pd(OH)2 (1 g) was added. The reaction was shaken at 45 psi H2 for 6 h and the catalyst was removed by filtration through Celite. The solution was concentrated in vacuo. The residue was azeotroped with CCl4 and was triturated with Et2O to provide the title amine (360 mg).

1. customThe catalyst was removed by filtration through Celite and additional Pd(OH)2 (1 g)
2. additionwas added
3. stirringThe reaction was shaken at 45 psi H2 for 6 h
4. customthe catalyst was removed by filtration through Celite
5. concentrationThe solution was concentrated in vacuo
6. customThe residue was azeotroped with CCl4
7. customwas triturated with Et2O