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HRID 201作成日:2026年10月23日

N-methyl-2-morpholin-4-ylacetamide → N-methyl-2-morpholin-4-yl-N-[6-(2-morpholin-4-yl-4-oxopyrido[1,2-a]pyrimidin-9-yl)dibenzothiophen-2-yl]acetamide

https://huagongshe.com/ja/reaction/201

反応式

関与物質

役割名称HCID仕込み量
反応物N-methyl-2-morpholin-4-ylacetamideHCID 22031405—
反応物[6-(2-Morpholin-4-yl-4-oxopyrido[1,2-a]pyrimidin-9-yl)dibenzothiophen-2-yl] trifluoromethanesulfonateHCID 87563685—
試薬Potassium Phosphate, TribasicHCID 62657—
触媒Binap, (A+-)-HCID 634876—
触媒Palladium (II) acetateHCID 4144353—
溶媒TolueneHCID 1140—
生成物N-methyl-2-morpholin-4-yl-N-[6-(2-morpholin-4-yl-4-oxopyrido[1,2-a]pyrimidin-9-yl)dibenzothiophen-2-yl]acetamideHCID 687589150%

反応条件

温度110 °C

反応手順

In a microwave vial, under nitrogen, at room temperature, a solution of 6-(2-morpholino-4-oxo-4H-pyrido[1,2-a]pyrimidin-9-yl)dibenzo[b,d]thiophen-2-yl trifluoromethanesulfonate (63 mg, 0.11 mmol) in dry toluene (1 mL) was added to a stirred mixture of N-methyl-2-morpholinoacetamide (35.5 mg, 0.22 mmol), Tripotassium phosphate (47.6 mg, 0.22 mmol), rac BINAP (6.99 mg, 0.01 mmol) and Palladium(II) acetate (2.52 mg, 0.01 mmol) in . The resulting mixture was heated in a Biotage Optimiser Microwave reactor under nitrogen at 100 °C for 3 hours. UPLC of the reaction showed no indication of the desired compound - not isolated - reaction abandonned.

情報源と証拠

出典データセット750 AstraZeneca ELN dataset
ORD IDord-cddf8b0bbaa34d7fad426cd90b95c72f
出典メモ750 AstraZeneca ELN dataset