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HRID 68937作成日:2026年10月25日

Triethyl methanetricarboxylate → 2-hydroxy-4-oxo-7-(5-trifluoromethyl-pyridin-2-yl)-5,6,7,8-tetrahydro-4H-9-thia-1,4a,7-triaza-fluorene-3-carboxylic acid ethyl ester

https://huagongshe.com/reaction/68937

反応式

関与物質

役割名称HCID仕込み量
反応物Triethyl methanetricarboxylateHCID 80471—
反応物5-(5-(Trifluoromethyl)pyridin-2-yl)-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridin-2-amineHCID 73555049—
溶媒O-XyleneHCID 7237—
生成物2-hydroxy-4-oxo-7-(5-trifluoromethyl-pyridin-2-yl)-5,6,7,8-tetrahydro-4H-9-thia-1,4a,7-triaza-fluorene-3-carboxylic acid ethyl esterHCID 13633777715.5%

反応条件

温度145 °C

反応手順

The mixture of 5-(5-trifluoromethyl-pyridin-2-yl)-4,5,6,7-tetrahydro-thiazolo[5,4-c]pyridin-2-ylamine (5.7 gm, 0.019 mol) and triethyl methantricarboxylate (16.1 ml, 0.076 mol) in xylene (100 ml) was heated at 140-150° C. for 6 hours. Xylene was evaporated and diethyl ether was then added and the suspension was stirred for 15 minutes. It was filtered and washed with ether. The crude solid was digested with dichloromethane (200 ml) and filtered to remove insoluble residue. Dichloromethane layer was distilled off under vacuum to give 1.3 gm of title compound.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US08822484B2
出典データセットuspto-grants-2014_09
ORD IDord-6e1bf009e1fe450b9247887b89e521b1
出典メモuspto-grants-2014_09