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HRID 219985作成日:2026年10月25日

2'-Ethyl-2-(methoxymethyl)-[1,1'-biphenyl]-4-carboxylic acid → Ethyl 4-(4-{5-[2'-ethyl-2-(methoxymethyl)biphenyl-4-yl]-1,2,4-oxadiazol-3-yl}-2-fluorophenoxy)butanoate

https://huagongshe.com/reaction/219985

反応式

関与物質

役割名称HCID仕込み量
反応物2'-Ethyl-2-(methoxymethyl)-[1,1'-biphenyl]-4-carboxylic acidHCID 59495809—
反応物Ethyl 4-{4-[amino(hydroxyimino)methyl]-2-fluorophenoxy}butanoateHCID 72307473—
生成物Ethyl 4-(4-{5-[2'-ethyl-2-(methoxymethyl)biphenyl-4-yl]-1,2,4-oxadiazol-3-yl}-2-fluorophenoxy)butanoateHCID 67528056—

反応手順

The title compound was prepared following procedure described for example 4, step 1, but starting from Intermediate 36 (202.74 mg; 0.75 mmol) and Intermediate 66 (234.54 mg; 0.83 mmol). The reaction mixture was filtered through a SPE NH2 column (10 g) and rinsed with ACN. The filtrate was passed through a SPE SCX column (10 g) and rinsed with ACN. After evaporation of the solvents, the crude product was purified by flash chromatography (c-hex/(DCM/EtOAc 1:1) gradient from 1:0 to 1:1), affording the title compound as a colorless oil. 1H NMR (CDCl3) δ 8.41 (d, J=1.3 Hz, 1H), 8.15 (dd, J=7.9, 1.8 Hz, 1H), 7.95-7.90 (m, 2H), 7.41-7.34 (m, 3H), 7.29-7.23 (m, 1H), 7.12-7.05 (m, 2H), 4.22-4.13 (m, 6H), 3.33 (s, 3H), 2.57 (t, J=7.2 Hz, 2H), 2.50-2.28 (m, 2H), 2.24-2.17 (m, 2H), 1.27 (t, J=7.2 Hz, 3H), 1.05 (t, J=7.5 Hz, 3H). LC/MS (Method B): 519.4 (M+H)+. HPLC (Method A) Rt 6.62 min (Purity: 99.9%).

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US08202865B2
出典データセットuspto-grants-2012_06
ORD IDord-34fc034bd8354dcf9f964c6716e64744
出典メモuspto-grants-2012_06