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HRID 45083作成日:2026年10月23日

5-Hydroxyindole → (+/-)-4-(1H-Indol-5-yloxy)-8-methyl-5,8-dihydro-6H-pyrido[3,4-d]pyrimidine-7-carboxylic acid tert-butyl ester

https://huagongshe.com/ja/reaction/45083

反応式

関与物質

役割名称HCID仕込み量
反応物5-HydroxyindoleHCID 16054—
反応物1,8-Diazabicyclo(5.4.0)undec-7-eneHCID 81184—
反応物tert-Butyl 4-chloro-8-methyl-5,8-dihydropyrido[3,4-d]pyrimidine-7(6H)-carboxylateHCID 59394669—
溶媒AcetonitrileHCID 6342—
生成物(+/-)-4-(1H-Indol-5-yloxy)-8-methyl-5,8-dihydro-6H-pyrido[3,4-d]pyrimidine-7-carboxylic acid tert-butyl esterHCID 59394465—

反応条件

温度80 °C

反応手順

To a solution of 4-chloro-8-methyl-5,8-dihydro-6H-pyrido[3,4-d]pyrimidine-7-carboxylic acid tert-butyl ester (228 mg, 0.80 mmol), 5-hydroxyindole (139 mg, 1.05 mmol) and MeCN (5 mL) is added DBU (0.15 mL, 1.05 mmol). The resulting misture is heated at 80° C. for 4 h. The reaction is then concentrated in vacuo and the residue separated via FCC (5-60% EtOAc/heptane). MS (ESI) m/z 381.1 (M+H).

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US08541432B2
出典データセットuspto-grants-2013_09
ORD IDord-d00b4fc61fe247708747fde4069fb94b
出典メモuspto-grants-2013_09