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HRID 546972作成日:2026年10月25日

Potassium Phosphate, Tribasic → [5-(4-{1-ethyl-1-[3-methyl-4-(1-trimethylsilanyloxy-cyclopentylethynyl)-phenyl]-propyl}-2-methyl-phenyl)-pyridin-3-yl]-acetic Acid Methyl Ester

https://huagongshe.com/reaction/546972

反応式

関与物質

役割名称HCID仕込み量
反応物Potassium Phosphate, TribasicHCID 62657—
反応物Methyl 2-(5-bromopyridin-3-yl)acetateHCID 23398394—
反応物2-(4-{1-Ethyl-1-[3-methyl-4-(1-trimethylsilanyloxy-cyclopentylethynyl)-phenyl]-propyl}-2-methyl-phenyl)-4,4,5,5-tetramethyl-[1,3,2]dioxaborolaneHCID 57708976—
溶媒DimethylformamideHCID 6228—
生成物[5-(4-{1-ethyl-1-[3-methyl-4-(1-trimethylsilanyloxy-cyclopentylethynyl)-phenyl]-propyl}-2-methyl-phenyl)-pyridin-3-yl]-acetic Acid Methyl EsterHCID 5770918567.8%

反応条件

温度140 °C

反応手順

A solution of 2-(4-{1-ethyl-1-[3-methyl-4-(1-trimethylsilanyloxy-cyclopentylethynyl)-phenyl]-propyl}-2-methyl-phenyl)-4,4,5,5-tetramethyl-[1,3,2]dioxaborolane (Example 32-(4); 54.1 mg, 0.0968 mmol), (5-bromo-pyridin-3-yl)acetic acid methyl ester (Example 24-(2); 33.4 mg, 0.14 mmol), tetrakistriphenylphosphine palladium (15.6 mg, 0.0135 mmol) and potassium phosphate (30.8 mg, 0.14 mmol) in N,N-dimethylformamide (0.27 mL) was stirred with microwave heating at 140° C. for 10 minutes. The reaction mixture was filtered through cotton plug, and the mixture was purified by silica gel chromatography (45% ethyl acetate/hexane) to give the title compound (38.2 mg, 67%).

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US07935688B2
出典データセットuspto-grants-2011_05
ORD IDord-7c92ea82fd88468ba71dc0f4aeebe33e
出典メモuspto-grants-2011_05