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Bromotrimethylsilane → Tenofovir
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Bromotrimethylsilane | HCID 76113 | — |
| 反応物 | Diethyl P-(((1R)-2-(6-amino-9H-purin-9-yl)-1-methylethoxy)methyl)phosphonate | HCID 10947889 | — |
| 溶媒 | Acetonitrile | HCID 6342 | — |
| 生成物 | Tenofovir | HCID 464205 | — |
反応手順
To a reaction vessel was added stepwise the product (D) of step (4), acetonitrile and Bromotrimethylsilane, the mixture was refluxed while stirring until the completion of the reaction, volatile liquid was removed under vacuum, the resultant residue was then dissolved in a suitable amount of water, and the resulting solution was adjusted to pH 3.0˜3.5 to give the product 9-[(R)-2-(phosphonomethoxy)propyl]adenine (PMPA). Furthermore, dichloromethane or chloroform could be used as reaction solvent and iodotrimethylsilane or chlorotrimethylsilane/potassium iodide as the deprotection agent.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US08507463B2 |
| 出典データセット | uspto-grants-2013_08 |
| ORD ID | ord-8714acba1ab1429395fcb886b63619c7 |
| 出典メモ | uspto-grants-2013_08 |