참여 물질
| 역할 | 이름 | HCID | 투입량 |
|---|
| 반응물 | Methanol | HCID 887 | — |
| 반응물 | Acetic Anhydride | HCID 7918 | — |
| 반응물 | Triethylamine | HCID 8471 | — |
| 반응물 | Desacetyl famciclovir hydrochloride | HCID 44226540 | — |
| 촉매 | 4-(Dimethylamino)pyridine | HCID 14284 | — |
| 용매 | Isopropanol | HCID 3776 | — |
| 용매 | Dichloromethane | HCID 6344 | — |
| 생성물 | Famciclovir | HCID 3324 | 70% |
반응 단계
To a stirred suspension of 2-amino-9-(4-hydroxy-3-hydroxymethylbut-1-yl)purine hydrochloride (0.79 g), 4-dimethylaminopyridine (16 mg) and triethylamine (1.4 ml) in dichloromethane (16 ml) at room temperature was added acetic anhydride (0.57 ml). The resulting mixture was stirred at ambient temperature for 2.25 hours. Methanol (4 ml) was added and the solution stirred for 0.5 hours before being evaporated to dryness. Water (20 ml) was added and the aqueous solution extracted with dichloromethane (3×20 ml). The combined extracts were concentrated to give an oil. This oil was dissolved in 2-propanol (5 ml), the solvent evaporated and the residue recrystallised from 2-propanol (5 ml). The product was collected by filtration, washed with 2-propanol (3 ml) and dried to give the title compound (654 mg, 70%).
출처 및 근거
| DOI | 10.6084/m9.figshare.5104873.v1 |
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| 특허 번호 | US06806375B2 |
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| 출처 데이터셋 | uspto-grants-2004_10 |
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| ORD ID | ord-9ad1f9c441df42e1884e9625e9eeaff8 |
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| 출처 메모 | uspto-grants-2004_10 |
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