Huagongshe화공사 화학 정보 인쇄 보고서 · 연구 참고용
Dimethylformamide → Tenofovir
참여 물질
| 역할 | 이름 | HCID | 투입량 |
|---|---|---|---|
| 반응물 | Dimethylformamide | HCID 6228 | — |
| 반응물 | 9-(2-Hydroxypropyl)adenine, (R)- | HCID 445211 | — |
| 반응물 | Diethyl P-[[[(4-methylphenyl)sulfonyl]oxy]methyl]phosphonate | HCID 4193599 | — |
| 반응물 | Magnesium 2-methylpropan-2-olate | HCID 12040442 | — |
| 용매 | 1,2-Dichloroethane | HCID 11 | — |
| 용매 | Acetic Acid | HCID 176 | — |
| 용매 | Water | HCID 962 | — |
| 용매 | Chloroform | HCID 6212 | — |
| 용매 | Dichloromethane | HCID 6344 | — |
| 생성물 | Tenofovir | HCID 464205 | — |
반응 단계
Accordingly (R)-9-[2-(hydroxyl)propyl]adenine is condensed with Diethyl p-toluene sulfonyloxy methylphosphonate in presence of Magnesium tert-butoxide in a polar solvent preferably dimethylformamide at a temperature of 70° C. to 80° C. After the reaction completion the reaction mass is neutralized by adding an acid preferably acetic acid and the solvent is distilled off completely. The obtained crude is dissolved in a chlorinated hydrocarbon selected from Methylenedichloride, chloroform, and Ethylene dichloride and water is added. The reaction mixture is filtered to remove the salts and Methylenedichloride layer is separated. Methylenedichloride is distilled off completely to get (R)-9-[2-(phosphonomethoxy)propyl]adenine.
출처 및 근거
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 특허 번호 | US08049009B2 |
| 출처 데이터셋 | uspto-grants-2011_11 |
| ORD ID | ord-1c01f1b6a05443549967b3ba56551380 |
| 출처 메모 | uspto-grants-2011_11 |