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HRID 229722作成日:2026年10月26日

1-Ethyl-3-(3'-dimethylaminopropyl)carbodiimide → 5-(N-(tert-butoxycarbonyl)-L-alanyl)oxy-7-methyl-3-(3-trifluoromethylphenyl)-5,6,7,8-tetrahydrocinnoline

https://huagongshe.com/reaction/229722

反応式

関与物質

役割名称HCID仕込み量
反応物1-Ethyl-3-(3'-dimethylaminopropyl)carbodiimideHCID 15908—
反応物Tert-butoxycarbonylalanineHCID 85082—
反応物7-Methyl-3-(3-(trifluoromethyl)phenyl)-5,6,7,8-tetrahydrocinnolin-5-olHCID 9972528—
溶媒DichloromethaneHCID 6344—
溶媒TetrahydrofuranHCID 8028—
生成物5-(N-(tert-butoxycarbonyl)-L-alanyl)oxy-7-methyl-3-(3-trifluoromethylphenyl)-5,6,7,8-tetrahydrocinnolineHCID 68844509—

反応手順

7-Methyl-3-(3-trifluoromethylphenyl)-5,6,7,8-tetrahydrocinnolin-5-ol (10 mg, 0.03 mmol) obtained in Example 6 was dissolved in a mixed solvent of tetrahydrofuran and dichloromethane (0.5 mL. 0.5 mL), followed by adding N-ethyl-N′-(3-dimethylaminopropyl)carbodiimide (9 mg, 0.045 mmol), N,N-dimethylaminopyridine (catalytic amount) and N-(tert-butoxycarbonyl)-L-alanine (9 mg, 0.045 mmol) and stirring at room temperature over night. After completion of the reaction, the reaction liquid was concentrated and thus obtained residue was purified using silica gel column chromatography (hexane/ethyl acetate=1/1) to obtain an objective compound.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US07563893B2
出典データセットuspto-grants-2009_07
ORD IDord-17dc1c9c39fe4caa8b43c4efcbfec233
出典メモuspto-grants-2009_07