HOAt → 4-[(4-aminopyrimidine-5-yl)carbonyl]amino-N-(2,6-dichlorobenzoyl)-L-phenylalanine methylester

HRID 1393064노트

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HRID 1393064 반응식
[CH3:1][O:2][C:3](=[O:24])[C@H:4]([CH2:16][C:17]1[CH:22]=[CH:21][C:20]([NH2:23])=[CH:19][CH:18]=1)[NH:5][C:6](=[O:15])[C:7]1[C:12]([Cl:13])=[CH:11][CH:10]=[CH:9][C:8]=1[Cl:14].C(Cl)CCl.Cl.C1C=NC2N(O)N=NC=2C=1.[NH2:40][C:41]1[C:46]([C:47](O)=[O:48])=[CH:45][N:44]=[CH:43][N:42]=1>ClCCl.C(N(CC)CC)C>[CH3:1][O:2][C:3](=[O:24])[C@H:4]([CH2:16][C:17]1[CH:18]=[CH:19][C:20]([NH:23][C:47]([C:46]2[C:41]([NH2:40])=[N:42][CH:43]=[N:44][CH:45]=2)=[O:48])=[CH:21][CH:22]=1)[NH:5][C:6](=[O:15])[C:7]1[C:8]([Cl:14])=[CH:9][CH:10]=[CH:11][C:12]=1[Cl:13]

참가 물질

7

반응물 4

HCID 181649HOAtHCID 12014404-Aminopyrimidine-5-carboxylic acidHCID 10384309HCID 10384309, 화합물HCID 22619321HCID 22619321, 화합물

생성물 1

HCID 866008844-[(4-aminopyrimidine-5-yl)carbonyl]amino-N-(2,6-dichlorobenzoyl)-L-phenylalanine methylester수율 10.9%

시약·촉매·용매 2

HCID 6344Dichloromethane용매2회HCID 8471Triethylamine용매

실험 절차

The mixture of N-(2,6-dichlorobenzoyl)-4-amino-L-phenylalanine methylester (1.0 g), EDC/HCl (783 mg), HOAt (555 mg), triethylamine (747 μL), 4-aminopyrimidine-5-carboxylic acid (417 mg) and dichloromethane (15 mL) was stirred overnight. After diluting the mixture with dichloromethane and washing with saturated sodium bicarbonate water, the organic layer thereof was dried over sodium sulfate and concentrated. The residue was washed with dichloromethane to obtain 145 mg of a crude material of the title compound.

후처리

  1. washwashing with saturated sodium bicarbonate water
  2. dry with materialthe organic layer thereof was dried over sodium sulfate
  3. concentrationconcentrated
  4. washThe residue was washed with dichloromethane

출처 및 근거

ORD 기록
ord-6f06c3795ed5412bb11bdd15724223b0
출처 데이터셋
uspto-grants-2008_03
특허 번호
US07345049B2

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