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HRID 245069作成日:2026年10月26日

2-Amino-1-methylcyclopentanol hydrochloride → 2-Chloro-4-{[(1r,2r)-2-Hydroxy-2-Methylcyclopentyl]amino}-3-Methylbenzonitrile

https://huagongshe.com/reaction/245069

反応式

関与物質

役割名称HCID仕込み量
反応物2-Amino-1-methylcyclopentanol hydrochlorideHCID 19818423—
反応物2-Chloro-4-fluoro-3-methylbenzonitrileHCID 44550971—
生成物2-Chloro-4-{[(1r,2r)-2-Hydroxy-2-Methylcyclopentyl]amino}-3-MethylbenzonitrileHCID 71543393—
生成物2-Chloro-4-[[2-hydroxy-2-methyl-cyclopentyl]amino]-3-methyl-benzonitrileHCID 78105364—

反応手順

2-Chloro-4-[[2-hydroxy-2-methyl-cyclopentyl]amino]-3-methyl-benzonitrile is prepared essentially as described in Example 1 using 2-amino-1-methyl-cyclopentanol, hydrochloride and 2-chloro-4-fluoro-3-methyl-benzonitrile. The crude material was purified using silica gel chromatography (25-55% EtOAc/hexane) to obtain Diastereomer 1 (0.54 g) and Diastereomer 2 (1.56 g). Diastereomer 2 is assigned trans configuration based on co-crystal with AR.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US08658693B2
出典データセットuspto-grants-2014_02
ORD IDord-5df85959ada949869ff13aace4cd962f
出典メモuspto-grants-2014_02