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HRID 69595作成日:2026年10月24日

Diisopropylethylamine → (S)-N-methyl-4-(4-((6-oxo-5,6,6a,7,8,9-hexahydropyrido[3,2-e]pyrrolo[1,2-a]pyrazin-3-yl)methyl)piperazin-1-yl)benzamide

https://huagongshe.com/ja/reaction/69595

反応式

関与物質

役割名称HCID仕込み量
反応物DiisopropylethylamineHCID 81531—
反応物(Cyanomethyl)trimethylphosphanium iodideHCID 10514344—
反応物N-methyl-4-(piperazin-1-yl)benzamideHCID 28749530—
反応物(S)-3-(hydroxymethyl)-6a,7,8,9-tetrahydropyrido[3,2-e]pyrrolo[1,2-a]pyrazin-6(5H)-oneHCID 58324378—
溶媒Dimethyl SulfoxideHCID 679—
溶媒PropionitrileHCID 7854—
生成物(S)-N-methyl-4-(4-((6-oxo-5,6,6a,7,8,9-hexahydropyrido[3,2-e]pyrrolo[1,2-a]pyrazin-3-yl)methyl)piperazin-1-yl)benzamideHCID 58324415—

反応条件

温度90 °C

反応手順

(S)-3-(hydroxymethyl)-6a,7,8,9-tetrahydropyrido[3,2-e]pyrrolo[1,2-a]pyrazin-6(5H)-one (1.500 g, 6.84 mmol), N-methyl-4-(piperazin-1-yl)benzamide (1.500 g, 6.84 mmol), (cyanomethyl)trimethylphosphonium iodide (2.494 g, 10.26 mmol) and N,N-diisopropylethylamine (5.97 ml, 34.2 mmol) were suspended in propiononitrile (Volume: 27.4 ml) and heated in a closed vial at 90° C. The crude reaction was cooled to RT, DMSO (1 ml) was added, and the mixture was purified via HPLC (55-90, basic) to give the product as a white solid.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US08822470B2
出典データセットuspto-grants-2014_09
ORD IDord-325bc05ae51642279bcd9c58c77c1c4b
出典メモuspto-grants-2014_09