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HRID 600808作成日:2026年10月26日

2-azido-1-(4-methylphenyl)ethanone → [8-(5-p-Methylphenyloxazol-2-ylamino)-1,2,3,4-tetrahydronaphthalen-2-yl]carbamic acid tert-butyl ester

https://huagongshe.com/reaction/600808

反応式

関与物質

役割名称HCID仕込み量
反応物2-azido-1-(4-methylphenyl)ethanoneHCID 11008439—
反応物HCID 53416493HCID 53416493—
反応物2-Ethoxy-8-isothiocyanato-1,4-dihydronaphthaleneHCID 86609612—
反応物HCID 86609614HCID 86609614—
生成物[8-(5-p-Methylphenyloxazol-2-ylamino)-1,2,3,4-tetrahydronaphthalen-2-yl]carbamic acid tert-butyl esterHCID 6722928683%

反応手順

The title compound was prepared using the procedure as described in Example 1H, substituting the product of Example 20F (188 mg, 0.618 mmol) for the product of Example 1F and the product of Example 9A (130 mg, 0.741 mmol) for the product of Example 1G. The crude product was purified by flash chromatography eluting with 2% to 5% CH3OH/CH2Cl2 followed by 60% EtOAc/hexanes which gave 215 mg (83%) of the title compound as a yellow amorphous solid. 1H NMR (DMSO-d6) δ 9.06 (br s, 1H), 7.60 (d, J=7.8 Hz, 1H), 7.45 (d, J=8.1 Hz, 2H), 7.29 (s, 1H), 7.23 (d, J=8.1 Hz, 2H), 7.10 (t, J=7.8 Hz, 1H), 6.98 (br d, 1H), 6.84 (d, J=7.5 Hz, 1H), 3.65 (m, 1H), 3.02 (m, 1H), 2.83 (m, 2H), 2.42 (m, 1H), 2.31 (s, 3H), 1.87 (m, 1H), 1.58 (m, 1H), 1.39 (s, 9H); MS (ESI+) m/z 420 (M+H)+.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US07902236B2
出典データセットuspto-grants-2011_03
ORD IDord-f5c45e1305cd48baa4f5f170cd6b7dc1
出典メモuspto-grants-2011_03