참여 물질
| 역할 | 이름 | HCID | 투입량 |
|---|
| 반응물 | Piperidine | HCID 8082 | — |
| 반응물 | Tert-butyl 4-[(5-chloro-6-hydroxy-3-oxo-2,3-dihydrobenzofuran-7-yl)methyl]piperazine-1-carboxylate | HCID 71278506 | — |
| 반응물 | HCID 178520032 | HCID 178520032 | — |
| 용매 | Methanol | HCID 887 | — |
| 생성물 | HCID 178452319 | HCID 178452319 | 36.2% |
반응 단계
A solution of tert-butyl 4-[(5-chloro-6-hydroxy-3-oxo-2,3-dihydrobenzofuran-7-yl)methyl]piperazine-1-carboxylate (0.100 g, 0.261 mmol) synthesized in Example B13, Step 2 in methanol (1 mL) was added with 5-fluoro-1H-indazole-3-carbaldehyde (0.0428 g, 0.261 mmol) synthesized in Example B8, Step 3, and piperidine (0.00222 g, 0.0261 mmol) at room temperature, and the mixture was stirred at 60° C. for 1 hour. The reaction mixture was cooled to room temperature, then added with methanol (4 mL), and suspended in methanol and thereby washed to obtain tert-butyl (Z)-4-({5-chloro-2-[(5-fluoro-1H-indazol-3-yl)methylene]-6-hydroxy-3-oxo-2,3-dihydrobenzofuran-7-yl}methyl)piperazine-1-carboxylate (0.050 g, 36%).
출처 및 근거
| DOI | 10.6084/m9.figshare.5104873.v1 |
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| 특허 번호 | US09156827B2 |
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| 출처 데이터셋 | uspto-grants-2015_10 |
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| ORD ID | ord-986e9e3fe8494160afc389a07908726c |
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| 출처 메모 | uspto-grants-2015_10 |
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