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HRID 1945680作成日:2026年10月25日

Trifluoroacetic acid → 8-Azetidin-3-ylmethyl-2-(2-isopropylbenzoimidazol-1-yl)-9-methyl-6-morpholin-4-yl-9H-purine

https://huagongshe.com/reaction/1945680

反応式

関与物質

役割名称HCID仕込み量
反応物Trifluoroacetic acidHCID 6422—
反応物3-[2-(2-Isopropylbenzoimidazol-1-yl)-9-methyl-6-morpholin-4-yl-9H-purin-8-ylmethyl]azetidine-1-carboxylic acid tert-butyl esterHCID 59605629—
溶媒DichloromethaneHCID 6344—
生成物8-Azetidin-3-ylmethyl-2-(2-isopropylbenzoimidazol-1-yl)-9-methyl-6-morpholin-4-yl-9H-purineHCID 59605635—

反応手順

To a solution of 3-[2-(2-isopropylbenzoimidazol-1-yl)-9-methyl-6-morpholin-4-yl-9H-purin-8-ylmethyl]azetidine-1-carboxylic acid tert-butyl ester (256 mg, 0.47 mmol) in DCM (5 mL) was added TFA (5 mL) and the resulting mixture stirred for 2 h at r.t. The reaction mixture was loaded onto an Isolute® SCX-2 cartridge which was washed with MeOH/DCM and the product eluted with 2M NH3/MeOH affording the title compound as an orange foam (205 mg, 97%). LCMS (method H): RT 1.91 min [M+H]+ 447.4

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US08394796B2
出典データセットuspto-grants-2013_03
ORD IDord-c6f274ce9e274f84bf8778e45e02806f
出典メモuspto-grants-2013_03