Huagongshe화공사 화학 정보 인쇄 보고서 · 연구 참고용
Hydrochloric Acid → N-{3-[6-methyl-3-(2-{[3-(1-pyrrolidinylmethyl)phenyl]amino}-4-pyrimidinyl)pyrazolo[1,5-a]pyridin-2-yl]phenyl}-2-(2-thienyl)acetamide
참여 물질
| 역할 | 이름 | HCID | 투입량 |
|---|---|---|---|
| 반응물 | Hydrochloric Acid | HCID 313 | — |
| 반응물 | 3-(Pyrrolidin-1-ylmethyl)aniline | HCID 1096407 | — |
| 반응물 | N-{3-[3-(2-chloro-4-pyrimidinyl)-6-methylpyrazolo[1,5-a]pyridin-2-yl]phenyl}-2-(2-thienyl)acetamide | HCID 57737227 | — |
| 용매 | Isopropanol | HCID 3776 | — |
| 용매 | 1,4-Dioxane | HCID 31275 | — |
| 생성물 | N-{3-[6-methyl-3-(2-{[3-(1-pyrrolidinylmethyl)phenyl]amino}-4-pyrimidinyl)pyrazolo[1,5-a]pyridin-2-yl]phenyl}-2-(2-thienyl)acetamide | HCID 16749969 | 53.7% |
반응 단계
N-{3-[3-(2-chloro-4-pyrimidinyl)-6-methylpyrazolo[1,5-a]pyridin-2-yl]phenyl}-2-(2-thienyl)acetamide (100 mg, 0.22 mml), [3-(1-pyrrolidinylmethyl)phenyl]amine (46 mg, 0.26 mmol), and 4N HCl in dioxane (0.10 mL) were combined in i-PrOH (3 mL) in a procedure analogous to Example 67, Step B to afford the title compound as a yellow solid (70 mg, 53%). 1H NMR (300 MHz, DMSO-d6) δ 10.40 (s, 1H), 9.55 (s, 1H), 8.71 (s, 1H), 8.47 (d, J=9.8 Hz, 1H), 8.26 (d, J=5.3 Hz, 1H), 7.91 (s, 1H), 7.78 (d, J=7.7 Hz, 1H), 7.72-7.67 (m, 2H), 7.48-7.36 (m, 3H), 7.31-7.19 (m, 2H), 7.00-7.01 (m, 2H), 6.92 (d, J=7.5 Hz, 1H), 6.50 (d, J=5.6 Hz, 1H), 3.91 (s, 2H), 3.57 (s, 2H), 2.52-2.45 (m, 4H), 2.41 (s, 3H), 1.74-1.69 (m, 4H). ES-LC/MS m/z=600 [M+H]+.
출처 및 근거
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 특허 번호 | US07807673B2 |
| 출처 데이터셋 | uspto-grants-2010_10 |
| ORD ID | ord-0c19a51f30d64128937ec9c7a4e6c473 |
| 출처 메모 | uspto-grants-2010_10 |