化工社化工社 化学情報印刷レポート · 研究参考用
Acetic Anhydride → Abiraterone Acetate
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Acetic Anhydride | HCID 7918 | — |
| 反応物 | Abiraterone | HCID 132971 | — |
| 溶媒 | Triethylamine | HCID 8471 | — |
| 生成物 | Abiraterone Acetate | HCID 9821849 | — |
反応手順
In one embodiment of the invention, abiraterone is acetylated by using acetic anhydride in the presence of a base, preferably triethylamine, and purified in hexane and ethanol to give pure abiraterone acetate of formula (I) with an overall yield up to 43-45% from the DHEA and a high purity (up to 99.0% by HPLC). In this embodiment, charcoal and a chelating resin are advantageously added to the hexane and ethanol solution of abiraterone acetate; the reaction mixture is then filtered and the pure active ingredient is crystallized. Suitable chelating resins that can be used in the invention are immobilized resins such as complex phenol-formaldehyde based resins; the Hokuetsu brand type MA-A resin (available from Ajinomoto) being preferred.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US09353145B2 |
| 出典データセット | uspto-grants-2016_05 |
| ORD ID | ord-15b89b14420741f79eae02e35ab6bc75 |
| 出典メモ | uspto-grants-2016_05 |