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HRID 220519作成日:2026年10月26日

Acetic Acid → 3'-(4-Chlorophenyl)-4-(3,5-dimethyl-1-phenyl-1H-pyrazol-4-ylmethyl)-3,4,5,6-tetrahydro-2H-[1,2']bipyrazine hydrochloride

https://huagongshe.com/reaction/220519

反応式

関与物質

役割名称HCID仕込み量
反応物Acetic AcidHCID 176—
反応物Ammonium ChlorideHCID 25517—
反応物1H-Pyrazole-4-carboxaldehyde, 3,5-dimethyl-1-phenyl-HCID 89179—
反応物Sodium triacetoxyborohydrideHCID 5049666—
反応物2-(4-Chlorophenyl)-3-(piperazin-1-yl)pyrazineHCID 68594257—
溶媒1,2-DichloroethaneHCID 11—
生成物3'-(4-Chlorophenyl)-4-(3,5-dimethyl-1-phenyl-1H-pyrazol-4-ylmethyl)-3,4,5,6-tetrahydro-2H-[1,2']bipyrazine hydrochlorideHCID 6859554064.3%

反応手順

Couple 3′-(4-chlorophenyl)-3,4,5,6-tetrahydro-2H-[1,2′]bipyrazinyl (0.103 g, 0.400 mmol) and 3,5-dimethyl-1-phenyl 1H-pyrazole-4-carbaldehyde (0.083 g, 0.679 mmol) in the presence of acetic acid (0.035 mL, 0.61 mmol) and sodium triacetoxy-borohydride (0.105 g, 0.491 mmol) in DCE (5 mL) for 44 hr. Purify by silica gel chromatography, eluting with 0:100 to 10:90 methanol:DCM. Dissolve the free base in methanol and add ammonium chloride (6.0 mg, 0.2 mmol). Stir overnight, concentrate under reduced pressure, add diethyl ether and stir overnight. Isolate the solid product by filtration and vacuum dry overnight to give the title compound (0.0637 g, 46%). MS (ES): m/z=460 [M+H]+.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US08202873B2
出典データセットuspto-grants-2012_06
ORD IDord-19e2f948e9224b0982895768a13d3794
出典メモuspto-grants-2012_06