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Water → N-(Benzyloxycarbonyl)-L-aspartyl-L-phenylalanine methyl ester
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Water | HCID 962 | — |
| 反応物 | Methyl L-phenylalaninate hydrochloride | HCID 75736 | — |
| 反応物 | Sodium Acetate | HCID 517045 | — |
| 反応物 | (S)-Benzyl (tetrahydro-2,5-dioxo-3-furyl)carbamate | HCID 11128682 | — |
| 溶媒 | Acetic Acid | HCID 176 | — |
| 生成物 | N-(Benzyloxycarbonyl)-L-aspartyl-L-phenylalanine methyl ester | HCID 10159630 | 70.1% |
反応手順
In 100.4 g of acetic acid, 25.1 g (0.1 mole) of N-benzyloxycarbonyl-L-aspartic anhydride was suspended and 21.6 g (0.1 mole) of L-phenylalanine methyl ester hydrochloride was added at 10°-15° C. Successively 9.2 g (0.11 mole) of sodium acetate was added over 30 minutes at the same temperature. The reaction was carried out for 3 hours with stirring at the same temperature. Thereafter 75.3 g of water was added and cooled to 0°-5° C. Precipitated crystals were filtered, washed and dried. Crystals of N-benzyloxycarbonyl-α-L-aspartyl-L-phenylalanine methyl ester were obtained. The yield was 30.0 g (70.1% yield on L-phenylalanine methyl ester hydrochloride).
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US05302743 |
| 出典データセット | uspto-grants-1994_04 |
| ORD ID | ord-7b73544978204f3ba8f8803bbe568f34 |
| 出典メモ | uspto-grants-1994_04 |