참여 물질
| 역할 | 이름 | HCID | 투입량 |
|---|
| 반응물 | acetyl-DL-leucine | HCID 1995 | — |
| 반응물 | Isobutyl chloroformate | HCID 62365 | — |
| 반응물 | HCID 178507442 | HCID 178507442 | — |
| 용매 | Dimethylformamide | HCID 6228 | — |
| 용매 | Dichloromethane | HCID 6344 | — |
| 용매 | Triethylamine | HCID 8471 | — |
| 생성물 | HCID 178474741 | HCID 178474741 | 71.4% |
반응 단계
A solution of 13.0 g (75 mmol) of N-acetyl-DL-leucine, 10.5 ml (75 mmol) of triethylamine, and 150 ml of dichloromethane is stirred at -10° and 9.75 ml (75 mmol) of isobutyl chloroformate is added. The reaction mixture is stirred for 1/2 hour at -10° C. and a cold solution of 11.6 g (50 mmol) of 2-[4-aminophenyl)-4-hydroxy-5-pyrimidine carboxylic acid and 7.7 (55 mmol) of triethylamine in 200 ml of dimethylformamide is added. The mixture is stirred at 5° C. for 3 hrs and overnight at room temperature. The reaction mixture is evaporated and the residue treated with water. The pH is lowered to 2.5 with dilute hydrochloric acid and the solid filtered, washed with water, and dried to give 13.8 g of 2-[4-(N-acetyl-DL-leucylamino)phenyl]-4-hydroxy-5-pyrimidine carboxylic acid; mp 233°-235° C. dec.
출처 및 근거
| DOI | 10.6084/m9.figshare.5104873.v1 |
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| 특허 번호 | US04311699 |
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| 출처 데이터셋 | uspto-grants-1982_01 |
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| ORD ID | ord-fceb47acaddf4b658971068ab3942754 |
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| 출처 메모 | uspto-grants-1982_01 |
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