Bis(2-oxo-3-oxazolidinyl)phosphinic chloride → 1H-Benzoimidazole-2-carboxylic acid (1-pyrimidin-4-yl-piperidin-4-yl)-amide

HRID 18511

反応式

HRID 18511 の反応式
[NH:1]1[C:5]2[CH:6]=[CH:7][CH:8]=[CH:9][C:4]=2[N:3]=[C:2]1[C:10]([OH:12])=O.FC(F)(F)C(O)=O.[N:20]1[CH:25]=[CH:24][C:23]([N:26]2[CH2:31][CH2:30][CH:29]([NH2:32])[CH2:28][CH2:27]2)=[N:22][CH:21]=1.C1N(P(Cl)(N2C(=O)OCC2)=O)C(=O)OC1.C([O-])(O)=O.[Na+]>CN(C=O)C.CCN(CC)CC>[N:20]1[CH:25]=[CH:24][C:23]([N:26]2[CH2:27][CH2:28][CH:29]([NH:32][C:10]([C:2]3[NH:1][C:5]4[CH:6]=[CH:7][CH:8]=[CH:9][C:4]=4[N:3]=3)=[O:12])[CH2:30][CH2:31]2)=[N:22][CH:21]=1

参加物

7

反応物 4

HCID 152842Bis(2-oxo-3-oxazolidinyl)phosphinic chlorideHCID 2332402-Benzimidazolecarboxylic acidHCID 516892Sodium BicarbonateHCID 223943841-Pyrimidin-4-yl-piperidin-4-ylamine trifluoroacetate

生成物 1

HCID 860098671H-Benzoimidazole-2-carboxylic acid (1-pyrimidin-4-yl-piperidin-4-yl)-amide

試薬・触媒・溶媒 2

HCID 6228Dimethylformamide溶媒HCID 8471Triethylamine溶媒

実験手順

To a solution of 80 mg 1H-Benzoimidazole-2-carboxylic acid in 1 mL DMF and 0.2 mL NEt3, 200 mg 1-Pyrimidin-4-yl-piperidin-4-ylamine trifluoroacetate and 125 mg BOP-Cl were added and the mixture was stirred for 3 h. Finally, 3 mL saturated NaHCO3 solution were added and the mixture was filtered through a chem elut® cartridge by elution with ethyl acetate. After removal of the solvent under reduced pressure the crude product was subjected to the next reaction step without further purification. Yield: 160 mg.

後処理

  1. filtrationthe mixture was filtered through a chem elut® cartridge by elution with ethyl acetate
  2. customAfter removal of the solvent under reduced pressure the crude product
  3. customwas subjected to the next reaction step without further purification

出典と根拠

ORDレコード
ord-79f71b05143e49688872fd3f6a5d773c
出典データセット
uspto-grants-2010_06
特許番号
US07741341B2

関連ノート

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