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HRID 42359作成日:2026年10月25日

Trifluoroacetic acid → HCID 44622554、化合物

https://huagongshe.com/reaction/42359

反応式

関与物質

役割名称HCID仕込み量
反応物Trifluoroacetic acidHCID 6422—
反応物Mafenide HydrochlorideHCID 67313—
反応物DiisopropylethylamineHCID 81531—
反応物[2-Chloro-6-(4-fluoro-phenyl)-pyrido[3,2-d]pyrimidin-4-yl]-(1-trifluoromethyl-cyclopropyl)-amineHCID 58275477—
溶媒N-methyl-2-pyrrolidoneHCID 13387—
生成物HCID 44622554HCID 4462255450.1%

反応条件

温度140 °C

反応手順

A mixture of [2-Chloro-6-(4-fluoro-phenyl)-pyrido[3,2-d]pyrimidin-4-yl]-(1-trifluoromethyl-cyclopropyl)-amine (51.6 mg) and 4-aminomethyl-benzenesulfonamide hydrochloride (51.4 mg) was dissolved in NMP (1 mL) and treated with diisopropylethylamine (0.065 mL). The reaction mixture was sealed and heated by microwave to 140° C. for 1.5 h. The reaction mixture was cooled and purified by preparative HPLC (5-95% acetonitrile:water with 0.1% TFA) to afford 36 mg (41% yield) of the title compound as its TFA which was characterized by its NMR and mass spectrum as follows: 1H NMR (d6-DMSO): d 1.26 (br s, 2H), 1.37 (br s, 2H), 4.80 (d, 2H), 7.34-7.40 (m, 4H), 7.55 (d, 2H), 7.78 (d, 2H), 7.99 (d, 1H), 8.48 (m, 3H), 8.9 (br s, 1H), 10.1 (br s, 1H); MS (m/z): 533.2 ([M+H]+, 100).

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US08536187B2
出典データセットuspto-grants-2013_09
ORD IDord-9e3b2b283d9c441bb17f011cd5d90186
出典メモuspto-grants-2013_09