Huagongshe화공사 화학 정보 인쇄 보고서 · 연구 참고용
1,2-Dichloroethane → 1-[4-(Pyrimidin-2-ylaminomethyl)-piperidin-1-yl]4-thiophen-2-yl-butan-1-one
참여 물질
| 역할 | 이름 | HCID | 투입량 |
|---|---|---|---|
| 반응물 | 1,2-Dichloroethane | HCID 11 | — |
| 반응물 | Piperidine | HCID 8082 | — |
| 반응물 | 1-Hydroxybenzotriazole | HCID 75771 | — |
| 반응물 | 4-(2-Thienyl)Butyric Acid | HCID 78386 | — |
| 반응물 | Benzyl 4-[(2-pyrimidinylamino)methyl]-1-piperidinecarboxylate | HCID 9923385 | — |
| 용매 | Dimethylformamide | HCID 6228 | — |
| 생성물 | 1-[4-(Pyrimidin-2-ylaminomethyl)-piperidin-1-yl]4-thiophen-2-yl-butan-1-one | HCID 22135671 | — |
반응 단계
Benzyl 4-[(2-pyrimidinylamino)methyl]-1-piperidinecarboxylate (EXAMPLE 16) was hydrogenated as described in EXAMPLE 30, Step 1. The resulting piperidine was combined with EDC (1.3 equiv.), HOBT (1.0 equiv.), and 4-thiophen-2-yl-butyric acid (1.0 equiv.) in DMF and stirred for 2 h. The resulting reaction solution was partitioned into ethyl acetate and aqueous sodium bicarbonate. The organic layer was seperated and washed with pH 4.5 citric acid buffer (10% citric acid and sodium hydroxide), dried (sodium sulfate), and concentrated to yield the desired 1-[4-(pyrimidin-2-ylaminomethyl)-piperidin-1-yl]-4-thiophen-2-yl-butan-1-one. M.S. (M+1): 345.25.
출처 및 근거
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 특허 번호 | US07053089B2 |
| 출처 데이터셋 | uspto-grants-2006_05 |
| ORD ID | ord-8dcdaf91dbe64bf3bea6fcb554481fdb |
| 출처 메모 | uspto-grants-2006_05 |