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Ether, bis(1-chloroethyl) → N-benzoyl-O-(1-ethoxyethyl)-3-phenyl-isoserine
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Ether, bis(1-chloroethyl) | HCID 23419 | — |
| 反応物 | 3-Benzoylamino-2-hydroxy-3-phenyl-propionic acid | HCID 3315046 | — |
| 溶媒 | Dichloromethane | HCID 6344 | — |
| 生成物 | N-benzoyl-O-(1-ethoxyethyl)-3-phenyl-isoserine | HCID 67714526 | — |
反応手順
The epoxide of the cis-cinnamate is then regioselectively opened to produce 3-phenyl isoserinamide. This 3-phenyl isoserinamide is hydrolyzed to produce 3-phenyl-isoserine, which in turn is reacted with benzoyl chloride to form N-benzoyl-3-phenyl-isoserine. Next, the N-benzoyl-3-phenyl-isoserine is reacted with 1-chloroethyl ether and a tertiary amine in methylene chloride to form N-benzoyl-O-(1-ethoxyethyl)-3-phenyl-isoserine. Then, N-benzoyl-O-(1-ethoxyethyl)-3-phenyl-isoserine is reacted with the alcohol shown below: ##STR8## This resulting intermediate is converted to taxol by hydrolytically removing the 1-ethoxyethyl and triethylsilyl protecting groups.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US05663393 |
| 出典データセット | uspto-grants-1997_09 |
| ORD ID | ord-9b71bf70ef614f7191b2f7e2a5cc8913 |
| 出典メモ | uspto-grants-1997_09 |