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HRID 714130作成日:2026年10月26日

Trifluoroacetic acid → N-{2-[(3S)-3-amino-4-{[tert-butyl(diphenyl)silyl]oxy}butyl]phenyl}-Nalpha-(methoxycarbonyl)-beta-phenyl-L-phenylalaninamide

https://huagongshe.com/reaction/714130

反応式

関与物質

役割名称HCID仕込み量
反応物Trifluoroacetic acidHCID 6422—
反応物methyl[(2S)-1-({2-[(3S)-3-[(tert-butoxycarbonyl)amino]-4-{[tert-butyl(diphenyl)silyl]oxy}butyl]phenyl}amino)-1-oxo-3,3-diphenylpropan-2-yl]carbamateHCID 68029329—
溶媒DichloromethaneHCID 6344—
生成物N-{2-[(3S)-3-amino-4-{[tert-butyl(diphenyl)silyl]oxy}butyl]phenyl}-Nalpha-(methoxycarbonyl)-beta-phenyl-L-phenylalaninamideHCID 6802933095.4%

反応手順

Compound methyl[(2S)-1-({2-[(3S)-3-[(tert-butoxycarbonyl)amino]-4-{[tert-butyl(diphenyl)silyl]oxy}butyl]phenyl}amino)-1-oxo-3,3-diphenylpropan-2-yl]carbamate (7, 305.4 mg, 0.382 mmol) was dissolved in a cold mixture of DCM (3 ml) and TFA (1 mL, 12.98 mmol) and the final solution stirred at 0° C. for 1.5 h, quenched at 0° C. by slow addition of saturated NaHCO3, then diluted with DCM, washed with saturated NaHCO3, dried over MgSO4, filtered and concentrated to afford 255 mg (95% yield) of the title compound as white foam submitted to the next step without further purification. MS: m/z=700.3 (MH+).

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US09187415B2
出典データセットuspto-grants-2015_11
ORD IDord-3611c099fa244568bbe91520b1ecf4b6
出典メモuspto-grants-2015_11