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HRID 394025作成日:2026年10月26日

Dimethylformamide → (2r)-1-{(2s,4s)-4-Acetoxy-1-(3,3,3-triphenylpropanoyl)pyrrolidin-2-yl}carbonyl-n-{((3r)-1-cyclohexylmethyl-3-piperidyl)methyl}pyrrolidine-2-carboxamide

https://huagongshe.com/reaction/394025

反応式

関与物質

役割名称HCID仕込み量
反応物DimethylformamideHCID 6228—
反応物(2R)-N-{((3R)-1-cyclohexylmethyl-3-piperidyl)methyl}-1-{(2S,4R)-4-(methylsulfonyloxy)-1-(3,3,3-triphenylpropanoyl)pyrrolidin-2-yl}carbonylpyrrolidine-2-carboxyamideHCID 131724629—
触媒Tetrabutylammonium AcetateHCID 82707—
溶媒Ethyl AcetateHCID 8857—
生成物(2r)-1-{(2s,4s)-4-Acetoxy-1-(3,3,3-triphenylpropanoyl)pyrrolidin-2-yl}carbonyl-n-{((3r)-1-cyclohexylmethyl-3-piperidyl)methyl}pyrrolidine-2-carboxamideHCID 12149972—

反応手順

A solution of 40 mg of (2R)-N-{((3R)-1-cyclohexylmethyl-3-piperidyl)methyl}-1-{(2S,4R)-4-(methylsulfonyloxy)-1-(3,3,3-triphenylpropanoyl)pyrrolidin-2-yl}carbonylpyrrolidine-2-carboxyamide and 30 mg of tetrabutylammonium acetate in 1 ml of N,N-dimethylformamide was stirred at 85° C. for 15 hours under heating. The reaction liquid was diluted with ethyl acetate, successively washed with water and saturated brine, and dried over anhydrous sodium sulfate. The solvent was distilled off under reduced pressure, and the resulting residue was purified with a preparative thin-layer chromatography (Kieselgel™ 60F254, Art. 5744 (Merck), chloroform/methanol/28% aqueous ammonia=100/8/1), to provide 14 mg of the title compound as a colorless oily substance.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US06809108B1
出典データセットuspto-grants-2004_10
ORD IDord-8ce7075e514b496193cfb7e61b49b8a1
出典メモuspto-grants-2004_10