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HRID 1738913作成日:2026年10月25日

Triethylamine → (2R,4S)-N-[1-(3,5-Bis-trifluoromethyl-benzoyl)-2-benzyl-piperidin-4-yl]-quinazoline-4-carboxamide

https://huagongshe.com/reaction/1738913

反応式

関与物質

役割名称HCID仕込み量
反応物TriethylamineHCID 8471—
反応物Bis(2-oxo-3-oxazolidinyl)phosphinic chlorideHCID 152842—
反応物(2R,4S)-2-benzyl-1-(3,5-bis-(trifluoromethyl)benzoyl)-4-piperidinamineHCID 22869971—
反応物Quinazoline-4-carboxylic acidHCID 23008716—
溶媒DichloromethaneHCID 6344—
生成物(2R,4S)-N-[1-(3,5-Bis-trifluoromethyl-benzoyl)-2-benzyl-piperidin-4-yl]-quinazoline-4-carboxamideHCID 18392943—

反応手順

Analogously to Example 1, 252 mg (1.45 mmol) of (2R,4S)-2-benzyl-1-(3,5-bis-trifluoromethyl-benzoyl)-4-piperidineamine in 5 ml of methylene chloride are reacted with 368 mg (1.45 mmol) of bis(2-oxo-3-oxazolidinyl)phosphinic acid chloride, 440 mg (4.35 mmol) of triethylamine and 566 mg (1.32 mmol) of quinazoline-4-carboxylic acid. The title compound is obtained in the form of white crystals. M.p.: 92-172° C.; TLC: hexane/ethyl acetate (1:1) Rf =0.37, FD-MS: M+ =586; [alpha]D=+1.3 (c=0.98, methylene chloride). ##STR16##

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US05965562
出典データセットuspto-grants-1999_10
ORD IDord-80a2adb8846940f9ae3bfcc6e0193f32
出典メモuspto-grants-1999_10