反应详情

360 mg (0.7 mmol) of methyl (S)-3-(3′-{[(1-biphenyl-4-ylmethanoyl)methylamino]methyl}biphenyl-4-yl)-2-ethoxypropionate in 10 ml of THF are introduced into a round-bottomed flask. 60 mg (1.4 mmol) of lithium hydroxide monohydrate, 1 ml of water and 1 ml of methanol are added and the mixture is stirred for 4 hours. The reaction medium is poured into water, acidified to pH 1, extracted with ethyl acetate, the organic phase decanted off, dried over magnesium sulphate and evaporated off. The residue obtained is purified by chromatography on a silica column eluted with a heptane and ethyl acetate (50/50) mixture and 280 mg (80%) of (S)-3-(3′-{[(1-biphenyl-4-ylmethanoyl)methylamino]methyl}biphenyl-4-yl)-2-ethoxypropionic acid are obtained in the form of an amorphous white solid.

1. extractionextracted with ethyl acetate
2. customthe organic phase decanted off
3. dry with materialdried over magnesium sulphate
4. customevaporated off
5. customThe residue obtained
6. customis purified by chromatography on a silica column
7. washeluted with a heptane and ethyl acetate (50/50) mixture and 280 mg (80%) of (S)-3-(3′-{[(1-biphenyl-4-ylmethanoyl)methylamino]methyl}biphenyl-4-yl)-2-ethoxypropionic acid
8. customare obtained in the form of an amorphous white solid