Huagongshe화공사 화학 정보 인쇄 보고서 · 연구 참고용
2-Methyl-2-butanol → 2-[2,6-Difluoro-4-(1-hydroxy-1-methylethyl)phenyl]-5-{[5-(1-hydroxy-1-methylethyl)pyridin-2-yl]amino}-1,3-thiazole-4-carboxamide
참여 물질
| 역할 | 이름 | HCID | 투입량 |
|---|---|---|---|
| 반응물 | 2-Methyl-2-butanol | HCID 6405 | — |
| 반응물 | Potassium Carbonate | HCID 11430 | — |
| 반응물 | 2-Dicyclohexylphosphino-2',4',6'-triisoprophylbiphenyl | HCID 11155794 | — |
| 반응물 | 2-(6-Bromo-3-pyridyl)-2-propanol | HCID 22391973 | — |
| 반응물 | 5-Amino-2-[2,6-difluoro-4-(1-hydroxy-1-methylethyl)phenyl]-1,3-thiazole-4-carboxamide | HCID 58335271 | — |
| 촉매 | Bis(dibenzylideneacetone)palladium | HCID 9811564 | — |
| 생성물 | 2-[2,6-Difluoro-4-(1-hydroxy-1-methylethyl)phenyl]-5-{[5-(1-hydroxy-1-methylethyl)pyridin-2-yl]amino}-1,3-thiazole-4-carboxamide | HCID 57482804 | — |
반응 단계
The title compound was prepared as described in Example 15, Step 7 using 5-amino-2-[2,6-difluoro-4-(1-hydroxy-1-methylethyl)phenyl]-1,3-thiazole-4-carboxamide (Example 15, Step 5) (42 mg, 0.13 mmol), 2-(6-bromopyridin-3-yl)propan-2-ol (for preparation, see WO 2004/050024 A2 Example 120 Step A) (29 mg, 0.13 mmol), Pd2(dba)3 (12 mg, 0.013 mmol), X-PHOS (32 mg, 0.067 mmol), potassium carbonate (19 mg, 0.13 mmol), and tert-amyl alcohol (0.27 ml) as starting materials. 1H NMR (500 MHz, d6-DMSO) δ 11.31 (s, 1H), 8.40 (d, 1H), 7.83 (dd, 1H), 7.65 (s, 1H), 7.48 (s, 1H), 7.32 (d, 2H), 7.20 (d, 1H), 5.38 (s, 1H), 5.13 (s, 1H), 1.44 (s, 6H), 1.43 (s, 6H). LRMS (APCI) calc'd for C21H23F2N4O3S [M+H]+ 449.1, found 449.0.
출처 및 근거
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 특허 번호 | US08278335B2 |
| 출처 데이터셋 | uspto-grants-2012_10 |
| ORD ID | ord-08a89075738440b984fd96eab72a37cf |
| 출처 메모 | uspto-grants-2012_10 |