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HRID 486作成日:2026年10月24日

Morpholine → methyl 2-methyl-1-{[2-methyl-3-(trifluoromethyl)phenyl]methyl}-6-(4-morpholinyl)-1H-benzimidazole-4-carboxylate

https://huagongshe.com/ja/reaction/486

反応式

関与物質

役割名称HCID仕込み量
反応物MorpholineHCID 8083—
反応物HCID 178418216HCID 178418216—
試薬Potassium tert-butoxideHCID 23665647—
触媒TributylphosphineHCID 13831—
触媒Palladium (II) acetateHCID 4144353—
溶媒1,4-DioxaneHCID 31275—
生成物methyl 2-methyl-1-{[2-methyl-3-(trifluoromethyl)phenyl]methyl}-6-(4-morpholinyl)-1H-benzimidazole-4-carboxylateHCID 569598280%

反応手順

methyl 6-bromo-2-methyl-1-(2-methyl-3-(trifluoromethyl)benzyl)-1H-benzo[d]imidazole-4-carboxylate (441 mg, 1.00 mmol) was taken up with morpholine (435 µl, 5.00 mmol), potassium tert-butoxide (449 mg, 4.00 mmol), tri-n-butylphosphine (49.3 µl, 0.2 mmol) and palladium(II) acetate (22.44 mg, 0.10 mmol) in dioxane (10ml) and heated for 18 hrs at 100°C. The reaction profile showed no required product and only dimer adduct to be present. the reaction was therefore abandoned.

情報源と証拠

出典データセット750 AstraZeneca ELN dataset
ORD IDord-f93da8755d504800bf04ba573750bf86
出典メモ750 AstraZeneca ELN dataset