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HRID 2053531作成日:2026年10月26日

2-(2-Fluorophenyl)ethylamine → tert-butyl (4S,5R)-2-[2-(2-fluorophenyl)ethylamino]-4,5-diphenyl-4,5-dihydroimidazole-1-carboxylate

https://huagongshe.com/reaction/2053531

反応式

関与物質

役割名称HCID仕込み量
反応物2-(2-Fluorophenyl)ethylamineHCID 643357—
反応物cis-4,5-Diphenyl-2-methylthio-4,5-dihydro-imidazole-1-carboxylic Acid, Tert-Butyl EsterHCID 86596320—
溶媒MethanolHCID 887—
生成物tert-butyl (4S,5R)-2-[2-(2-fluorophenyl)ethylamino]-4,5-diphenyl-4,5-dihydroimidazole-1-carboxylateHCID 6857067543.2%

反応条件

温度100 °C

反応手順

A mixture of intermediate 59 (0.5 g, 1.36 mmol), 2-fluorophenethylamine (0.531 mL, 4.07 mmol) and MeOH (0.1 mL) is heated at 100° C. for 3 days. The reaction mixture is cooled to RT, and is purified by chromatography on silica gel; gradient elution with heptane:EtOAc (70:30-60:40) gives 0.27 g of the product 91. 1H NMR (CDCl3) δ 7.40-6.85 (m, 13H), 6.80-6.65 (m, 2H), 5.45-5.25 (m, 2H), 3.90-3.60 (m, 2H), 1.15 (s, 9H); MS: m/z 460 (M++1).

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US07326792B2
出典データセットuspto-grants-2008_02
ORD IDord-a51d4890194d4f4bb726fd1f7be3b579
出典メモuspto-grants-2008_02