Huagongshe화공사 화학 정보 인쇄 보고서 · 연구 참고용
Binap, (A+-)- → benzyl (1S,5S)-6-(5,6-dichloro-3-pyridinyl)-3,6-diazabicyclo[3.2.0]heptane-3-carboxylate
참여 물질
| 역할 | 이름 | HCID | 투입량 |
|---|---|---|---|
| 반응물 | Binap, (A+-)- | HCID 634876 | — |
| 반응물 | 2,3-Dichloro-5-iodopyridine | HCID 21892874 | — |
| 반응물 | benzyl (1S,5S)-3,6-diazabicyclo[3.2.0]heptane-3-carboxylate | HCID 23635906 | — |
| 반응물 | Sodium t-butoxide | HCID 23676156 | — |
| 촉매 | Bis(dibenzylideneacetone)palladium | HCID 9811564 | — |
| 생성물 | benzyl (1S,5S)-6-(5,6-dichloro-3-pyridinyl)-3,6-diazabicyclo[3.2.0]heptane-3-carboxylate | HCID 23636393 | 25% |
반응 단계
The product of Example 52D (451 mg, 1.94 mmol) was coupled with 2,3-dichloro-5-iodopyridine (805 mg, 2.94 mmol; U.S. Pat. No. 7,733,912) using tris(dibenzylideneacetone)dipalladium (Pd2(dba)3, 36 mg, 0.039 mmol; Alfa Aesar), 2,2′-bis(diphenylphosphino)-1,1′-binaphthyl (BINAP, 82 mg, 0.13 mmol; Strem), and sodium tert-butoxide (360 mg, 3.75 mmol; Aldrich) according to the procedure described in Example 1E to provide the title compound (184 mg, 25% yield). MS (DCI/NH3) m/z 378, 380 (M+H)+.
출처 및 근거
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 특허 번호 | US06809105B2 |
| 출처 데이터셋 | uspto-grants-2004_10 |
| ORD ID | ord-de44466960434d609637616073c4b386 |
| 출처 메모 | uspto-grants-2004_10 |