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HRID 1916722作成日:2026年10月27日

Triphenylphosphine → 5-(4-Chloro-phenyl)-2-[3-(4-pyrrolidin-1-ylmethyl-phenoxy)-prop-1-ynyl]-pyridine

https://huagongshe.com/reaction/1916722

反応式

関与物質

役割名称HCID仕込み量
反応物TriphenylphosphineHCID 11776—
反応物Diisopropyl diazene-1,2-dicarboxylateHCID 75555—
反応物4-(Pyrrolidin-1-ylmethyl)phenolHCID 18771978—
反応物3-[5-(4-Chloro-phenyl)-pyridin-2-yl]-prop-2-yn-1-olHCID 69076337—
溶媒TetrahydrofuranHCID 8028—
生成物5-(4-Chloro-phenyl)-2-[3-(4-pyrrolidin-1-ylmethyl-phenoxy)-prop-1-ynyl]-pyridineHCID 59835746—

反応手順

131 mg (0.5 mmol) triphenylphosphane are added to a solution of 100 mg (0.41 mmol) 3-[5-(4-chloro-phenyl)-pyridin-2-yl]-prop-2-yn-1-ol and 88 mg (0.5 mmol) 4-pyrrolidin-1-ylmethyl-phenol in 4 mL THF. Then 0.1 mL (0.5 mmol) diisopropyl azo-dicarboxylate is slowly added dropwise and the reaction mixture is stirred for 3 h at RT. The mixture is evaporated down i. vac., the residue is taken up in 1 mL DMF and purified by HPLC. The product obtained, which still contains triphenylphosphane oxide, is again purified by chromatography (silica gel, EtOAc after EtOAc/MeOH/NH3 9:1:0.1).

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US08618132B2
出典データセットuspto-grants-2013_12
ORD IDord-f08aa4f833cf41098db3611a2b4d8708
出典メモuspto-grants-2013_12