Huagongshe화공사 화학 정보 인쇄 보고서 · 연구 참고용
Cesium carbonate → Methyl cis(+/-)-5-(4-{[(benzyloxy)carbonyl]amino}-3-methoxypiperidin-1-yl)-3-methylthiophene-2-carboxylate
참여 물질
| 역할 | 이름 | HCID | 투입량 |
|---|---|---|---|
| 반응물 | Cesium carbonate | HCID 10796 | — |
| 반응물 | Binap, (A+-)- | HCID 634876 | — |
| 반응물 | Methyl 5-bromo-3-methylthiophene-2-carboxylate | HCID 53438912 | — |
| 반응물 | Benzyl cis(+/-)-[3-methoxypiperidin-4-yl]carbamate | HCID 86648490 | — |
| 촉매 | palladium(II) acetate | HCID 167845 | — |
| 생성물 | Methyl cis(+/-)-5-(4-{[(benzyloxy)carbonyl]amino}-3-methoxypiperidin-1-yl)-3-methylthiophene-2-carboxylate | HCID 86648826 | 23.6% |
반응 단계
The same operation as in Example (244b) was performed using methyl 5-bromo-3-methylthiophene-2-carboxylate obtained in Example (245a) (218 mg, 0.93 mmol), benzyl cis(±)-(3-methoxypiperidin-4-yl)-carbamate obtained in Example (40b) (270 mg, 1.02 mmol), palladium acetate (42 mg, 0.19 mmol), BINAP (115 mg, 0.19 mmol) and cesium carbonate (423 mg, 1.30 mmol), to obtain 92 mg of the title compound as a yellow oily substance (24%).
출처 및 근거
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 특허 번호 | US08536197B2 |
| 출처 데이터셋 | uspto-grants-2013_09 |
| ORD ID | ord-9f771965f51343cb83a6d86cf4b28fbe |
| 출처 메모 | uspto-grants-2013_09 |