反应详情

N-(Benzyloxycarbonyl)-D-leucyl-L-leucine methyl ester (Example 29A, 1.12 g, 2.85 mmol) is provided at 0° C. in THF/water 2:1 (15 ml) and then lithium hydroxide monohydrate (140 mg, 5.71 mmol, 2 equivalents) is added. When the HPLC chromatogram (Method 2) shows complete conversion (about 1 h), the reaction mixture is adjusted to pH 3-4 with acetic acid, concentrated in vacuo under cold conditions and then freed of solvent by freeze-drying overnight. The crude product is purified by means of preparative HPLC (Method 13) whereby 958 mg (88.7% of theory) of the title compound are obtained.

1. customconversion (about 1 h)
2. concentrationconcentrated in vacuo under cold conditions
3. customby freeze-drying overnight
4. customThe crude product is purified by means of preparative HPLC (Method 13) whereby 958 mg (88.7% of theory) of the title compound
5. customare obtained