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HRID 1043578作成日:2026年10月26日

2-(propan-2-yl)-1H-1,3-benzodiazole → tert-butyl 3-((2-(2-isopropyl-1H-benzo[d]imidazol-1-yl)-4-morpholinopyrido[3,2-d]pyrimidin-6-yl)methylene)azetidine-1-carboxylate

https://huagongshe.com/reaction/1043578

反応式

関与物質

役割名称HCID仕込み量
反応物2-(propan-2-yl)-1H-1,3-benzodiazoleHCID 22121—
反応物Sodium t-butoxideHCID 23676156—
反応物Tert-butyl 3-((2-chloro-4-morpholinopyrido[3,2-d]pyrimidin-6-yl)methylene)azetidine-1-carboxylateHCID 58404986—
触媒palladium(II) acetateHCID 167845—
触媒HCID 178418851HCID 178418851—
生成物tert-butyl 3-((2-(2-isopropyl-1H-benzo[d]imidazol-1-yl)-4-morpholinopyrido[3,2-d]pyrimidin-6-yl)methylene)azetidine-1-carboxylateHCID 58404996—

反応手順

To a microwave vial was added tert-butyl 3-((2-chloro-4-morpholinopyrido[3,2-d]pyrimidin-6-yl)methylene)azetidine-1-carboxylate, 2-isopropyl-1H-benzo[d]imidazole (1.05 eq), sodium tert-butoxide (2 eq), Palladium Acetate (0.1 eq) and Bis(tri-t-butylphosphine)palladium (0.1 eq). The tube was flushed with nitrogen for 10 minutes before adding Toluene (8 mL). The reaction was microwaved at 145° C. for 20 minutes. The crude was purified by flash column chromatography to afford 0.22 g of tert-butyl 3-((2-(2-isopropyl-1H-benzo[d]imidazol-1-yl)-4-morpholinopyrido[3,2-d]pyrimidin-6-yl)methylene)azetidine-1-carboxylate.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US08563540B2
出典データセットuspto-grants-2013_10
ORD IDord-99d2f0aa561148f4a52780051186b385
出典メモuspto-grants-2013_10