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HRID 2426546作成日:2026年10月27日

5-Amino-4,6-dichloropyrimidine → 6-Chloro-N4-[1-(3,5-diisopropoxy-benzyl)-piperidin-4-yl]-pyrimidine-4,5-diamine

https://huagongshe.com/reaction/2426546

反応式

関与物質

役割名称HCID仕込み量
反応物5-Amino-4,6-dichloropyrimidineHCID 79434—
反応物1-(3,5-Diisopropoxy-benzyl)-piperidin-4-ylamineHCID 59210370—
溶媒AcetonitrileHCID 6342—
溶媒DiisopropylethylamineHCID 81531—
生成物6-Chloro-N4-[1-(3,5-diisopropoxy-benzyl)-piperidin-4-yl]-pyrimidine-4,5-diamineHCID 8661853720%

反応手順

A solution of 4,6-dichloro-pyrimidin-5-ylamine (19.7 mg, 0.12 mmol, 1.0 equiv; commercially available) and 1-(3,5-diisopropoxy-benzyl)-piperidin-4-ylamine (46.0 mg, 0.15 mmol, 1.25 equiv; intermediate A3) in N-ethyl diisopropylamine (1.0 mL) and acetonitril (1.0 mL) was heated by microwave irradiation to 160° C. for 20 min. Removal of the solvent under reduced pressure and purification by preparative HPLC on reversed phase eluting with a gradient of acetonitrile/water provided 10.6 mg (20%) of the title compound. MS (ISP): 434.3 [M+H]+.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US07968568B2
出典データセットuspto-grants-2011_06
ORD IDord-49a1894631f44386924bbbfc2a93bacc
出典メモuspto-grants-2011_06