関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|
| 反応物 | Dimethyl Sulfone | HCID 6213 | — |
| 反応物 | Chloroformamidinium chloride | HCID 3084509 | — |
| 反応物 | methyl 2-Acetamido-3-[2-[(2R)-2-[[3-(4-aminophenyl)benzoyl]amino]-4-benzyloxycarbonylbutoxy]-4-cyanophenyl]acrylate Trifluoroacetate | HCID 69142761 | — |
| 溶媒 | Water | HCID 962 | — |
| 生成物 | HCID 178499878 | HCID 178499878 | — |
反応手順
A mixture of 340 mg (0.52 mmol) of methyl 2-acetamido-3-[2-[(2R)-2-[[3-(4-aminophenyl)benzoyl]amino]-4-benzyloxycarbonylbutoxy]-4-cyanophenyl]acrylate trifluoroacetate, 430 mg (3.74 mmol) of chloroformamidine hydrochloride and 2.0 g of dimethyl sulfone was stirred at 120° C. for 2 hours. Water was added to the reaction mixture. After washing with ethyl acetate, the aqueous layer was freeze-dried and purified by the reversed phase HPLC in the same manner as that in step 5 in Example 1 to obtain the title compound.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|
| 特許番号 | US06710056B2 |
|---|
| 出典データセット | uspto-grants-2004_03 |
|---|
| ORD ID | ord-08fbdee52c4a49f6a3a13adebffe294a |
|---|
| 出典メモ | uspto-grants-2004_03 |
|---|
