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HRID 1502502作成日:2026年10月26日

Diisopropylethylamine → 8-methyl-2-phenyl-3-((1S)-1-(9-(tetrahydro-2H-pyran-2-yl)-9H-purin-6-ylamino)ethyl)-isoquinolin-1(2H)-one

https://huagongshe.com/reaction/1502502

反応式

関与物質

役割名称HCID仕込み量
反応物DiisopropylethylamineHCID 81531—
反応物6-chloro-9-(tetrahydro-2H-pyran-2-yl)-9H-purineHCID 97740—
反応物8-methyl-2-phenyl-3-((1S)-1-(9-(tetrahydro-2H-pyran-2-yl)-9H-purin-6-ylamino)ethyl)-isoquinolin-1(2H)-oneHCID 58008558—
反応物(S)-3-(1-aminoethyl)-8-methyl-2-phenylisoquinolin-1(2H)-oneHCID 58008747—
溶媒1-ButanolHCID 263—
生成物8-methyl-2-phenyl-3-((1S)-1-(9-(tetrahydro-2H-pyran-2-yl)-9H-purin-6-ylamino)ethyl)-isoquinolin-1(2H)-oneHCID 5800855860%
生成物HCID 178423766HCID 178423766—

反応手順

3-(1-Aminoethyl)-8-methyl-2-phenylisoquinolin-1(2H)-one (compound 4704) (200 mg, 0.72 mmol), 6-chloro-9-(tetrahydro-2H-pyran-2-yl)-9H-purine (344 mg, 1.44 mmol) and DIPEA (279 mg, 2.16 mmol) were dissolved in n-BuOH (20 ml), and the resulting mixture was stirred at reflux for 16 h. The reaction mixture was concentrated in vacuo and purified by flash column chromatography on silica gel (eluting with 30% to 50% Hex/EA) to afford the desired product, 8-methyl-2-phenyl-3-((1S)-1-(9-(tetrahydro-2H-pyran-2-yl)-9H-purin-6-ylamino)ethyl)-isoquinolin-1(2H)-one (compound 4901) (207 mg, 60% yield) as a white solid.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US09206182B2
出典データセットuspto-grants-2015_12
ORD IDord-4c7112b5cc384001a1e18cea96c36a8d
出典メモuspto-grants-2015_12