Pyridine → n-(Benzoyl)-3-hydroxylmethyl-n'-[(7-methoxycarbonyl-indol-3-yl)-oxoacetyl]-piperazine

HRID 992358

반응식

HRID 992358 반응식
OC[C:3]1[CH:4]=[C:5]([CH:14]=[CH:15][CH:16]=1)[C:6]([N:8]1[CH2:13][CH2:12][NH:11][CH2:10][CH2:9]1)=[O:7].FC(F)(F)[C:19](=N[Si](C)(C)C)[O:20][Si](C)(C)C.[CH3:32][O:33][C:34]([C:36]1[CH:37]=[CH:38][CH:39]=[C:40]2[C:44]=1[NH:43][CH:42]=[C:41]2[C:45](=[O:49])[C:46](Cl)=[O:47])=[O:35].N1C=CC=CC=1>C(#N)C>[C:6]([N:8]1[CH2:9][CH2:10][N:11]([C:46](=[O:47])[C:45]([C:41]2[C:40]3[C:44](=[C:36]([C:34]([O:33][CH3:32])=[O:35])[CH:37]=[CH:38][CH:39]=3)[NH:43][CH:42]=2)=[O:49])[CH:12]([CH2:19][OH:20])[CH2:13]1)(=[O:7])[C:5]1[CH:4]=[CH:3][CH:16]=[CH:15][CH:14]=1

참가 물질

6

반응물 4

HCID 1049PyridineHCID 94358Bis(trimethylsilyl)trifluoroacetamideHCID 18412093(7-Methoxycarbonyl-indol-3-yl)-oxoacetyl chlorideHCID 185197513-Hydroxylmethyl-benzoylpiperazine

생성물 1

HCID 18412084n-(Benzoyl)-3-hydroxylmethyl-n'-[(7-methoxycarbonyl-indol-3-yl)-oxoacetyl]-piperazine

시약·촉매·용매 1

HCID 6342Acetonitrile용매

실험 절차

To a stirred solution of 3-hydroxylmethyl-benzoylpiperazine XLIX (8.0 mg, 0.036 mmol) in acetonitrile (5 ml) was added BSTFA (8.1 mg, 0.036 mmol). After stirring for 30 minutes at room temperature, (7-methoxycarbonyl-indol-3-yl)-oxoacetyl chloride (8.1 mg, 0.036 mmol) and pyridine (0.5 ml) were added. The reaction was stirred for another 2 hours at room temperature. Concentration under vaccum provided a residue, which was then purified by Shimazu HPLC purification system to give 2 mg of N-(benzoyl)-3-hydroxylmethyl-N′-[(7-methoxycarbonyl-indol-3-yl)-oxoacetyl]-piperazine (Example 98).

후처리

  1. stirringThe reaction was stirred for another 2 hours at room temperature
  2. concentrationConcentration under vaccum
  3. customprovided a residue, which
  4. customwas then purified by Shimazu HPLC purification system

출처 및 근거

ORD 기록
ord-ba2a69e85db842e882cd61fc33b384e6
출처 데이터셋
uspto-grants-2002_10
특허 번호
US06469006B1

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