Huagongshe화공사 화학 정보 인쇄 보고서 · 연구 참고용
Cesium carbonate → Methyl cis(+/-)-3-(4-{[(benzyloxy)carbonyl]amino}-3-methoxypiperidin-1-yl)-5-fluorobenzoate
참여 물질
| 역할 | 이름 | HCID | 투입량 |
|---|---|---|---|
| 반응물 | Cesium carbonate | HCID 10796 | — |
| 반응물 | Binap, (A+-)- | HCID 634876 | — |
| 반응물 | Methyl 3-chloro-5-fluorobenzoate | HCID 21942504 | — |
| 반응물 | Benzyl cis(+/-)-[3-methoxypiperidin-4-yl]carbamate hydrochloride | HCID 86648698 | — |
| 촉매 | palladium(II) acetate | HCID 167845 | — |
| 생성물 | Methyl cis(+/-)-3-(4-{[(benzyloxy)carbonyl]amino}-3-methoxypiperidin-1-yl)-5-fluorobenzoate | HCID 86648729 | 34.5% |
반응 단계
The same operation as in Example (42a) was performed using benzyl cis(±)-[3-methoxypiperidin-4-yl]carbamate hydrochloride obtained in Example (160a) (165 mg, 0.55 mmol), methyl 3-chloro-5-fluorobenzoate (103 mg, 0.55 mmol), palladium acetate (12.3 mg, 0.05 mmol), BINAP (68.3 mg, 0.11 mmol) and cesium carbonate (536 mg, 1.65 mmol), to obtain 79 mg of the title compound as a yellow oily substance (35%).
출처 및 근거
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 특허 번호 | US08536197B2 |
| 출처 데이터셋 | uspto-grants-2013_09 |
| ORD ID | ord-25c3092eb6694f7fb6faac504b527022 |
| 출처 메모 | uspto-grants-2013_09 |