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HRID 1366626作成日:2026年10月27日

Triethylamine → Tris(1,1-dimethylethyl) 2-{2-chloro-5-fluoro-6-[(3-thienylmethyl)amino]-4-pyrimidinyl}-1,1,2-hydrazinetricarboxylate

https://huagongshe.com/reaction/1366626

反応式

関与物質

役割名称HCID仕込み量
反応物TriethylamineHCID 8471—
反応物3-ThiophenemethylamineHCID 2776381—
反応物Tris(1,1-dimethylethyl) 2-(2,6-dichloro-5-fluoro-4-pyrimidinyl)-1,1,2-hydrazinetricarboxylateHCID 58000755—
溶媒WaterHCID 962—
溶媒TetrahydrofuranHCID 8028—
生成物Tris(1,1-dimethylethyl) 2-{2-chloro-5-fluoro-6-[(3-thienylmethyl)amino]-4-pyrimidinyl}-1,1,2-hydrazinetricarboxylateHCID 8663700999.1%

反応手順

Tris(1,1-dimethylethyl)2-(2,6-dichloro-5-fluoro-4-pyrimidinyl)-1,1,2-hydrazinetricarboxylate (1.413 g, 2.85 mmol) was dissolved in THF (5 mL). To this solution was added triethylamine (0.48 mL, 3.4438 mmol), followed by commercially available (3-thienylmethyl)amine (0.322 g, 2.85 mmol) which was dissolved in THF (1 mL). After stirring, the reaction mixture was diluted with water, and the aqueous layer was extracted with ethyl acetate. The organics were dried (Na2SO4) and concentrated to produce tris(1,1-dimethylethyl)2-{2-chloro-5-fluoro-6-[(3-thienylmethyl)amino]-4-pyrimidinyl}-1,1,2-hydrazinetricarboxylate as a white solid (1.6214 g, 99%). LCMS: (M+H−3Boc)+=374.1.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US07893056B2
出典データセットuspto-grants-2011_02
ORD IDord-80beed6db33145ddb1d540651328e397
出典メモuspto-grants-2011_02