참여 물질
| 역할 | 이름 | HCID | 투입량 |
|---|
| 반응물 | Tert-Butyl nitrite | HCID 10906 | — |
| 반응물 | Antimony trifluoride | HCID 24554 | — |
| 반응물 | Amdoxovir | HCID 124088 | — |
| 반응물 | Acetonitrile--water (1/1) | HCID 18373917 | — |
| 용매 | Acetic Acid | HCID 176 | — |
| 용매 | dichloroethane DMSO | HCID 20230201 | — |
| 생성물 | 2'-Deoxy-2-fluoroadenosine | HCID 447864 | — |
반응 단계
DAPD (2 g, 7.5 mmol) was suspended in 170 mL dichloroethane/DMSO (4:1) and cooled to 0° C. under an inert atmosphere. To this is added antimony trifluoride (1.88 g, 10.5 mmol) and tert-butyl nitrite (1.85 ml, 1.6 g, 15.5 mmol) followed by stirring while allowing the reaction to warm to room temperature. Analysis of the reaction mixture by HPLC [Novapak C-18; 5% acetonitrile/water, 0.1M TEA, pH 7 with acetic acid] revealed a new peak which eluted at 6.4 min, indicating the synthesis of 2-fluoro-2′-deoxyadenosine with concomitant loss of starting material. The reaction was stirred overnight and quenched with triethylamine. The conversion to product by HPLC was 8%.
출처 및 근거
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|
| 특허 번호 | US06596858B2 |
|---|
| 출처 데이터셋 | uspto-grants-2003_07 |
|---|
| ORD ID | ord-c0cf169bbb1043559ffe654efb48d615 |
|---|
| 출처 메모 | uspto-grants-2003_07 |
|---|
