참여 물질
| 역할 | 이름 | HCID | 투입량 |
|---|
| 반응물 | Hydrochloric Acid | HCID 313 | — |
| 반응물 | 4,5-Dihydro-2-(methylthio)thiazole | HCID 88324 | — |
| 반응물 | Sodium Bicarbonate | HCID 516892 | — |
| 반응물 | N-(4-[2-(4-aminophenyl)ethyl]-5-[4-(methylsulfonyl)benzyl]-1,3-thiazol-2-yl)acetamide | HCID 21914845 | — |
| 용매 | 2-Methoxyethanol | HCID 8019 | — |
| 생성물 | HCID 21914702 | HCID 21914702 | 58.4% |
반응 단계
A mixture of N-{4-[2-(4-aminophenyl)ethyl]-5-[4-(methylsulfonyl)benzyl]-1,3-thiazol-2-yl}-acetamide (200 mg), 2-(methylsulfanyl)-4,5-dihydro-1,3-thiazole (62 mg), concentrated HCl (0.064 ml) and 2-methoxyethanol (3 ml) was stirred at 120° C. for 13 hours under N2 atmosphere. After cooled to r.t., the reaction mixture was made basic with saturated NaHCO3. The mixture was extracted with AcOEt. The organic layer was dried over anhydrous MgSO4, and concentrated in vacuo. The residue was purified by preparative silica gel chromatography with CHCl3/MeOH (10:1) as an eluent to give N-{4-{2-[4-(4,5-dihydro-1,3-thiazol-2-ylamino)phenyl]ethyl}-5-[4-(methylsulfonyl)benzyl]-1,3-thiazol-2-yl}acetamide (139.8 mg) as a pale yellow amorphous substance.
출처 및 근거
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|
| 특허 번호 | US07125901B2 |
|---|
| 출처 데이터셋 | uspto-grants-2006_10 |
|---|
| ORD ID | ord-5fe0962b202942d78d51b6145b462051 |
|---|
| 출처 메모 | uspto-grants-2006_10 |
|---|