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HRID 551962作成日:2026年10月27日

Cyclopropanecarboxaldehyde → Methyl 5-[(4-[(4-butylphenyl)ethynyl]benzyl) (cyclopropylmethyl)amino]-2-fluorobenzoate

https://huagongshe.com/reaction/551962

反応式

関与物質

役割名称HCID仕込み量
反応物CyclopropanecarboxaldehydeHCID 123114—
反応物Methyl 5-({4-[(4-butylphenyl)ethynyl]benzyl}amino)-2-fluorobenzoateHCID 11452740—
生成物Methyl 5-[(4-[(4-butylphenyl)ethynyl]benzyl) (cyclopropylmethyl)amino]-2-fluorobenzoateHCID 5755455954.6%

反応手順

The title compound was prepared following procedure described in example 23, step b) from methyl 5-({4-[(4-butylphenyl)ethynyl]benzyl}amino)-2-fluorobenzoate (326 mg; 0.78 mmol) and cyclopropanecarboxaldehyde (Aldrich, 87.94 μl; 1.18 mmol). Purification of the crude by preparative HPLC using a X-Terra column gave 200 mg (54%) of the title compound as a beige oil. HPLC, Rt: 5.91 min (purity: 99.7%), LC/MS, M+(ESI): 470.4, 1H NMR (CDCl3) δ: 7.66 (m, 1H), 7.39 (d, J=7.9 Hz, 4H), 7.00-7.17 (m, 6H), 4.62 (s, 2H), 3.93 (s, 3H), 3.44 (m, 3H), 2.59 (t, J=7.7 Hz, 2H), 1.57 (m, 2H), 1.31 (m, 2H), 0.90 (t, J=7.2 Hz, 3H), 0.53 (d, J=7.2 Hz, 2H), 0.24 (m, 2H).

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US07947851B2
出典データセットuspto-grants-2011_05
ORD IDord-bcd0f4891556468eb30e133a7f17f5a3
出典メモuspto-grants-2011_05