反应详情

To a solution of [1-[[[[3-[[(1,4-dihydro-6,7-dihydroxy-3-quinolinyl)carbonyl]amino]-2-oxo-1-imidazolidinyl]sulfonyl]amino]carbonyl]-2-oxo-3-azetidinyl]carbamic acid, phenylmethyl ester (3.35 g, 5.3 mmol) in 60 ml of N,N-dimethylformamide, N-methyl-N-trimethylsilyl trifluoroacetamide (5.28 g, 26.5 mmol) was added. After 30 minutes, 1.68 g of palladium on carbon was added, and the mixture was hydrogenolyzed for 1 hour. The catalyst was removed by filtration and the filtrate added to a solution of (Z)-2-amino-α-[[2-(diphenylmethoxy)-1,1-dimethyl-2-oxoethoxy]imino]-4-thiazoleacetic acid, 1-benzotriazole ester (2.96 g, 5.3 mmol) in 30 ml of N,N-dimethylformamide. After stirring for 20 hours, the solvent was distilled off and the residue triturated with 60 ml of water and 75 ml of ethyl acetate. The resulting crystals were filtered off, washed with water and dried in vacuo to give 3.27 g of the title compound.

1. waitthe mixture was hydrogenolyzed for 1 hour
2. customThe catalyst was removed by filtration
3. distillationthe solvent was distilled off
4. customthe residue triturated with 60 ml of water and 75 ml of ethyl acetate
5. filtrationThe resulting crystals were filtered off
6. washwashed with water
7. customdried in vacuo