참여 물질
| 역할 | 이름 | HCID | 투입량 |
|---|
| 반응물 | Triethylamine | HCID 8471 | — |
| 반응물 | Furan-2-sulfonyl Chloride | HCID 2795072 | — |
| 반응물 | (R)-(1-((2-amino-2,3-dihydro-1H-inden-5-yl)methyl)-3-(trifluoromethyl)-1H-pyrazol-4-yl)methanol | HCID 67026260 | — |
| 용매 | Dimethyl Sulfoxide | HCID 679 | — |
| 용매 | Tetrahydrofuran | HCID 8028 | — |
| 생성물 | HCID 67088095 | HCID 67088095 | 37.5% |
반응 단계
(R)-(1-((2-amino-2,3-dihydro-1H-inden-5-yl)methyl)-3-(trifluoromethyl)-1H-pyrazol-4-yl)methanol (0.08 mmol, 25 mg) was dissolved in tetrahydrofuran (1 mL) and triethylamine (0.25 mmol, 35 μL, 25 mg) followed by furan-2-sulfonyl chloride (0.084 mmol, 14.05 mg) and the solution stirred at room temperature overnight. The reaction was concentrated before partitioning between dichlormethane (3 mL) and 1N HCl. (3 mL). The organic layer was collected and dried using a hydrophobic frit and concentrated under a stream of nitrogen to give a brown residue which was dissolved in DMSO (1 mL) and purified on preparative basic HPLC to give (R)—N-(5-((4-(hydroxymethyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl)methyl)-2,3-dihydro-1H-inden-2-yl)furan-2-sulfonamide (13.1 mg, 0.03 mmol, 37.1%) MS (ESI): m/z [M+H]+ 442.2
출처 및 근거
| DOI | 10.6084/m9.figshare.5104873.v1 |
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| 특허 번호 | US08536214B2 |
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| 출처 데이터셋 | uspto-grants-2013_09 |
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| ORD ID | ord-78c13e640baa4b3cb2fd633cf8ea8f0a |
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| 출처 메모 | uspto-grants-2013_09 |
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