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HRID 249725作成日:2026年10月27日

Morpholine → 4-[5-(1,1-Dimethoxyethyl)-2-methoxy-3-trifluoromethylphenyl]morpholine

https://huagongshe.com/reaction/249725

反応式

関与物質

役割名称HCID仕込み量
反応物MorpholineHCID 8083—
反応物Binap, (A+-)-HCID 634876—
反応物1-Bromo-5-(1,1-dimethoxyethyl)-2-methoxy-3-trifluoromethylbenzeneHCID 58085697—
生成物4-[5-(1,1-Dimethoxyethyl)-2-methoxy-3-trifluoromethylphenyl]morpholineHCID 58085699—

反応手順

1-Bromo-5-(1,1-dimethoxyethyl)-2-methoxy-3-trifluoromethylbenzene (2 g) was initially introduced and argon was passed through with stirring for 0.5 h. Subsequently, the mixture was treated with Pd(II) acetate (13 mg), BINAP (54 mg) and sodium tertiary-butylate (784 mg), followed by morpholine (0.6 ml). The mixture obtained was stirred under argon at 85° C. for 8 h and after standing overnight at RT it was stirred at 85° C. for a further 8 h and allowed to stand overnight. The solvent was then stripped off and the residue was purified on silica gel (n-heptane-ethyl acetate gradient). 468 mg of the desired product were obtained.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US07863269B2
出典データセットuspto-grants-2011_01
ORD IDord-60483acf475248b1b8834088ccafcae2
出典メモuspto-grants-2011_01