Huagongshe화공사 화학 정보 인쇄 보고서 · 연구 참고용
Boron tribromide → [4-(2-Azepan-1-yl-ethoxy)-phenyl]-[2-(2,4-difluoro-phenyl)-6-hydroxy-naphthalen-1-yl]-methanone
참여 물질
| 역할 | 이름 | HCID | 투입량 |
|---|---|---|---|
| 반응물 | Boron tribromide | HCID 25134 | — |
| 반응물 | [4-(2-Azepan-1-yl-ethoxy)-phenyl]-[2-(2,4-difluoro-phenyl)-6-methoxy-naphthalen-1-yl]-methanone | HCID 11466453 | — |
| 반응물 | [2-(2,4-Difluoro-phenyl)-6-hydroxy-naphthalen-1-yl]-[4-(2-piperidin-1-yl-ethoxy)-phenyl]-methanone | HCID 67004951 | — |
| 생성물 | [4-(2-Azepan-1-yl-ethoxy)-phenyl]-[2-(2,4-difluoro-phenyl)-6-hydroxy-naphthalen-1-yl]-methanone | HCID 67004715 | 75% |
반응 단계
By the standard demethylation procedure found in the preparation of [2-(2,4-difluoro-phenyl)-6-hydroxy-naphthalen-1-yl]-[4-(2-piperidin-1-yl-ethoxy)-phenyl]-methanone, [4-(2-azepan-1-yl-ethoxy)-phenyl]-[2-(2,4-difluoro-phenyl)-6-methoxy-naphthalen-1-yl]-methanone (1.1 g, 2.1 mmol) is demethylated with BBr3 (1.0 mL, 10.5 mmol) to afford crude product. Purify on silica gel (0% to 5% methanol in methylene chloride) to yield 790 mg (75%) of the title compound: mass spectrum (ion spray) m/z=502.3 (M+H).
출처 및 근거
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 특허 번호 | US08217032B2 |
| 출처 데이터셋 | uspto-grants-2012_07 |
| ORD ID | ord-25b0df30719940b183b0d2d6c64253ce |
| 출처 메모 | uspto-grants-2012_07 |