6-[4-(2-tert-Butoxycarbonylamino-4-methylthiazole-5-carbonyl)-1-piperazinyl]-3,4-dihydro-2(1H)-quinolinone → 6-[4-(2-amino-4-methylthiazole-5-carbonyl)-1-piperazinyl]-3,4-dihydro-2(1H)-quinolinone

HRID 704635

반응식

HRID 704635 반응식
C(OC([NH:8][C:9]1[S:10][C:11]([C:15]([N:17]2[CH2:22][CH2:21][N:20]([C:23]3[CH:24]=[C:25]4[C:30](=[CH:31][CH:32]=3)[NH:29][C:28](=[O:33])[CH2:27][CH2:26]4)[CH2:19][CH2:18]2)=[O:16])=[C:12]([CH3:14])[N:13]=1)=O)(C)(C)C>C(O)=O>[NH2:8][C:9]1[S:10][C:11]([C:15]([N:17]2[CH2:18][CH2:19][N:20]([C:23]3[CH:24]=[C:25]4[C:30](=[CH:31][CH:32]=3)[NH:29][C:28](=[O:33])[CH2:27][CH2:26]4)[CH2:21][CH2:22]2)=[O:16])=[C:12]([CH3:14])[N:13]=1

참가 물질

3

반응물 1

HCID 200728916-[4-(2-tert-Butoxycarbonylamino-4-methylthiazole-5-carbonyl)-1-piperazinyl]-3,4-dihydro-2(1H)-quinolinone

생성물 1

HCID 200727936-[4-(2-amino-4-methylthiazole-5-carbonyl)-1-piperazinyl]-3,4-dihydro-2(1H)-quinolinone수율 95.2%

시약·촉매·용매 1

HCID 284Formic Acid용매

실험 절차

6-[4-(2-tert-Butoxycarbonylamino-4-methylthiazole-5-carbonyl)-1-piperazinyl]-3,4-dihydro-2(1H)-quinolinone (1.2 g) was dissolved in formic acid (25 ml) and the solution was stirred for 4 hours at ambient temperature. After the solvent was removed, ethyl acetate (10 ml) and water (10 ml) was added to the residue and the mixture was adjusted to pH 4.5 with 10% aqueous solution of potassium carbonate. The resulting precipitate was collected and recrystallized from methanol-water to give 6-[4-(2-amino-4-methylthiazole-5-carbonyl)-1-piperazinyl]-3,4-dihydro-2(1H)-quinolinone (0.9 g).

후처리

  1. customAfter the solvent was removed
  2. additionethyl acetate (10 ml) and water (10 ml) was added to the residue
  3. customThe resulting precipitate was collected
  4. customrecrystallized from methanol-water

출처 및 근거

ORD 기록
ord-5682d432bcc64531b954917cebff8033
출처 데이터셋
uspto-grants-1991_01
특허 번호
US04988698

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