Sodium borohydride → 1-[2-(3-Chlorophenyl)-2-hydroxyethyl]-4-[3,4-dihydro-2(1H)-quinazolinon-3-yl]-piperidine

HRID 67079

반응식

HRID 67079 반응식
[Cl:1][C:2]1[CH:3]=[C:4]([CH:25]=[CH:26][CH:27]=1)[C:5]([CH2:7][N:8]1[CH2:13][CH2:12][CH:11]([N:14]2[CH2:23][C:22]3[C:17](=[CH:18][CH:19]=[CH:20][CH:21]=3)[NH:16][C:15]2=[O:24])[CH2:10][CH2:9]1)=[O:6].[BH4-].[Na+]>CO>[Cl:1][C:2]1[CH:3]=[C:4]([CH:5]([OH:6])[CH2:7][N:8]2[CH2:9][CH2:10][CH:11]([N:14]3[CH2:23][C:22]4[C:17](=[CH:18][CH:19]=[CH:20][CH:21]=4)[NH:16][C:15]3=[O:24])[CH2:12][CH2:13]2)[CH:25]=[CH:26][CH:27]=1

참가 물질

4

반응물 2

HCID 4311764Sodium borohydrideHCID 127979921-(3-chlorobenzoylmethyl)-4-[3,4-dihydro-2(1H)-quinazolinon-3-yl]-piperidine

생성물 1

HCID 127979951-[2-(3-Chlorophenyl)-2-hydroxyethyl]-4-[3,4-dihydro-2(1H)-quinazolinon-3-yl]-piperidine수율 57.7%

시약·촉매·용매 1

HCID 887Methanol용매

실험 절차

In this example, 1.50 g of 1-(3-chlorobenzoylmethyl)-4-[3,4-dihydro-2(1H)-quinazolinon-3-yl]-piperidine and 75 ml of methanol are mixed and stirred at room temperature. To the stirred mixture, 1.0 g of sodium borohydride is added over a period of 5 hours. Then, the mixture is stirred overnight at room temperature. The white crystals deposited are separated by filtration, successively washed with methanol and water and dried to obtain 1.21 g of a crude product. The crude product is recrystallized from a mixed solvent of chloroform and ethanol to obtain 0.87 g of the desired product.

후처리

  1. stirringThen, the mixture is stirred overnight at room temperature
  2. customThe white crystals deposited are separated by filtration
  3. washsuccessively washed with methanol and water
  4. customdried
  5. customto obtain 1.21 g of a crude product
  6. customThe crude product is recrystallized from a mixed solvent of chloroform and ethanol

출처 및 근거

ORD 기록
ord-f4516bc0a6da42d782e6c4c4feee987e
출처 데이터셋
uspto-grants-1982_08
특허 번호
US04344948

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