Potassium Carbonate → 1-[1-{4-[5-(4-Amino-1-piperidinyl)pentoyloxy]benzoyl}-4-piperidinyl]-3,4-dihydrocarbostyril

HRID 1708318노트

반응식

HRID 1708318 반응식
FC(F)(F)C(NC1CCN(CCCCCO[C:18]2[CH:42]=[CH:41][C:21]([C:22]([N:24]3[CH2:29][CH2:28][CH:27]([N:30]4[C:40]5[C:35](=[CH:36][CH:37]=[CH:38][CH:39]=5)[CH2:34][CH2:33][C:31]4=[O:32])[CH2:26][CH2:25]3)=[O:23])=[CH:20][CH:19]=2)CC1)=O.[C:45](=[O:48])([O-])[O-:46].[K+].[K+]>CO>[NH2:30][CH:27]1[CH2:28][CH2:29][N:24]([CH2:22][CH2:21][CH2:20][CH2:19][C:45]([O:46][C:18]2[CH:42]=[CH:41][C:21]([C:22]([N:24]3[CH2:25][CH2:26][CH:27]([N:30]4[C:40]5[C:35](=[CH:36][CH:37]=[CH:38][CH:39]=5)[CH2:34][CH2:33][C:31]4=[O:32])[CH2:28][CH2:29]3)=[O:23])=[CH:20][CH:19]=2)=[O:48])[CH2:25][CH2:26]1

참가 물질

4

반응물 2

HCID 11430Potassium CarbonateHCID 189607451-[1-{4-[5-(4-Trifluoroacetylamino-1-piperidinyl)pentyloxy]benzoyl}-4-piperidinyl]-3,4-dihydrocarbostyril

생성물 1

HCID 572403741-[1-{4-[5-(4-Amino-1-piperidinyl)pentoyloxy]benzoyl}-4-piperidinyl]-3,4-dihydrocarbostyril수율 128.2%

시약·촉매·용매 1

HCID 887Methanol용매

실험 절차

1-[1-{4-[5-(4-Trifluoroacetylamino-1-piperidinyl)pentyloxy]benzoyl}-4-piperidinyl]-3,4-dihydrocarbostyril (1.8 g) is dissolved in methanol (40 ml), and thereto is added potassium carbonate (0.8 g). The mixture is stirred at room temperature overnight. The reaction solution is concentrated and thereto is added water. The mixture is extracted with chloroform, dried over sodium carbonate, and purified by silica gel column chromatography (eluent; dichloromethane:methanol=10:1) to give 1-[1-{4-[5-(4-amino-1-piperidinyl)pentoyloxy]benzoyl}-4-piperidinyl]-3,4-dihydrocarbostyril (1 g) as colorless oil.

후처리

  1. concentrationThe reaction solution is concentrated
  2. additionis added water
  3. extractionThe mixture is extracted with chloroform
  4. dry with materialdried over sodium carbonate
  5. custompurified by silica gel column chromatography (eluent; dichloromethane:methanol=10:1)

출처 및 근거

ORD 기록
ord-438adee7253744efbbc261e97762f74d
출처 데이터셋
uspto-grants-1994_10
특허 번호
US05356904

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