참여 물질
| 역할 | 이름 | HCID | 투입량 |
|---|
| 반응물 | Triethylamine | HCID 8471 | — |
| 반응물 | 1-Ethyl-3-(3'-dimethylaminopropyl)carbodiimide | HCID 15908 | — |
| 반응물 | 1-Hydroxybenzotriazole | HCID 75771 | — |
| 반응물 | 4-(2-((tert-Butoxycarbonyl)amino)ethoxy)benzoic acid | HCID 2755997 | — |
| 반응물 | HCID 178422083 | HCID 178422083 | — |
| 용매 | Dichloromethane | HCID 6344 | — |
| 생성물 | HCID 178453727 | HCID 178453727 | 412.1% |
반응 단계
A mixture of 2-((2S)-bicyclo[2.2.1]heptan-2-ylamino)-5-methyl-5-(piperidin-4-ylmethyl)thiazol-4(5H)-one (534 mg, 1.66 mmol), 4-[2-(Boc-amino)ethyloxy]-benzoic acid (NeoMPS, 701 mg, 2.49 mmol), EDCI (Aldrich, 637 mg, 3.32 mmol, 2.0 eq), HOBt (Aldrich, 45 mg, 0.332 mmol, 0.2 eq) and triethylamine (Aldrich, 336 mg, 3.32 mmol, 2.0 eq) in CH2Cl2 (10 mL) was stirred at room temperature for ca. 18 h. The reaction was quenched with saturated NaHCO3 (100 mL), and the crude product was extracted with CH2Cl2 (3×100 mL). The combined organic extracts were washed with brine, dried over Na2SO4, filtered, and concentrated. Flash column chromatography (silica gel, 0-5% MeOH in CH2Cl2) afforded the title compound as a white solid (800 mg). MS (ESI, pos. ion) m/z: 585 (M+H).
출처 및 근거
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|
| 특허 번호 | US08541592B2 |
|---|
| 출처 데이터셋 | uspto-grants-2013_09 |
|---|
| ORD ID | ord-8abc0d1e58874940854250353656a801 |
|---|
| 출처 메모 | uspto-grants-2013_09 |
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