Huagongshe화공사 화학 정보 인쇄 보고서 · 연구 참고용
HRID 76810생성일: 2026년 10월 24일
O-[(Ethoxycarbonyl)cyanomethylenamino]-N,N,N',N'-tetramethyluronium tetrafluoroborate → (s)-3-[5-(5-Chloro-thiophen-2-yl)-isoxazol-3-yl]-n-cyclopropylmethyl-2-[5-fluoro-2-methoxy-3-(2-oxo-piperidin-1-yl)-benzenesulfonylamino]-propionamide
https://huagongshe.com/ko/reaction/76810
참여 물질
| 역할 | 이름 | HCID | 투입량 |
|---|
| 반응물 | O-[(Ethoxycarbonyl)cyanomethylenamino]-N,N,N',N'-tetramethyluronium tetrafluoroborate | HCID 2733286 | — |
| 반응물 | N-Methylcyclopropanamine | HCID 11029756 | — |
| 반응물 | (s)-3-[5-(5-Chloro-thiophen-2-yl)-isoxazol-3-yl]-2-[5-fluoro-2-methoxy-3-(2-oxo-piperidin-1-yl)-benzenesulfonylamino]-propionic acid | HCID 66911181 | — |
| 생성물 | (s)-3-[5-(5-Chloro-thiophen-2-yl)-isoxazol-3-yl]-n-cyclopropylmethyl-2-[5-fluoro-2-methoxy-3-(2-oxo-piperidin-1-yl)-benzenesulfonylamino]-propionamide | HCID 66911141 | — |
반응 단계
Intermediate 17 (350 mg, 0.63 mmol) and cyclopropyl-methylamine (45 mg, 0.63 mmol) were coupled using the procedure described in example 1; 1.9), where only 25% conversion of starting materials was discovered. Heating to 50° C. did not lead to further conversion. Then TOTU (246 mg, 0.75 mmol) was added and after stirring for 1 h at RT conversion was completed. The mixture was purified by preparative HPLC. Yield after lyophilization: 162 mg, 43%, colorless, amorphous solid.
출처 및 근거
| DOI | 10.6084/m9.figshare.5104873.v1 |
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| 특허 번호 | US08835653B2 |
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| 출처 데이터셋 | uspto-grants-2014_09 |
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| ORD ID | ord-84bb71aa225b41fe8bf187851ad05c28 |
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| 출처 메모 | uspto-grants-2014_09 |
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