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

HRID 18507

反応式

HRID 18507 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.Cl.[CH:14]([N:17]1[CH2:22][CH2:21][CH:20]([NH2:23])[CH2:19][CH2:18]1)([CH3:16])[CH3:15].C1N(P(Cl)(N2C(=O)OCC2)=O)C(=O)OC1.C([O-])(O)=O.[Na+]>CN(C=O)C.CCN(CC)CC>[CH:14]([N:17]1[CH2:22][CH2:21][CH:20]([NH:23][C:10]([C:2]2[NH:1][C:5]3[CH:6]=[CH:7][CH:8]=[CH:9][C:4]=3[N:3]=2)=[O:12])[CH2:19][CH2:18]1)([CH3:16])[CH3:15]

参加物

7

反応物 4

HCID 152842Bis(2-oxo-3-oxazolidinyl)phosphinic chlorideHCID 2332402-Benzimidazolecarboxylic acidHCID 516892Sodium BicarbonateHCID 230334601-Isopropylpiperidin-4-amine hydrochloride

生成物 1

HCID 670127271H-Benzoimidazole-2-carboxylic acid (1-isopropyl-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 300 mg 1H-Benzoimidazole-2-carboxylic acid in 3 mL DMF and 1 mL NEt3, 398 mg 1-Isopropyl-piperidin-4-ylamine hydrochloride and 470 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.

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-be01ac0db92847d3925527deccc00814
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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