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HRID 475958作成日:2026年10月25日

1,2-Dichloroethane → N-[(6-Ethyl-4-methyl-2-oxo-1,2-dihydro-3-pyridinyl)methyl]-1-(1-methylethyl)-6-(4-pyridinyl)-1H-pyrazolo[3,4-b]pyridine-4-carboxamide

https://huagongshe.com/reaction/475958

反応式

関与物質

役割名称HCID仕込み量
反応物1,2-DichloroethaneHCID 11—
反応物Trifluoroacetic acidHCID 6422—
反応物4-MethylmorpholineHCID 7972—
反応物HOAtHCID 181649—
反応物1-(1-Methylethyl)-6-(4-pyridinyl)-1H-pyrazolo[3,4-b]pyridine-4-carboxylic acidHCID 20114625—
反応物HCID 67124323HCID 67124323—
溶媒DimethylformamideHCID 6228—
生成物N-[(6-Ethyl-4-methyl-2-oxo-1,2-dihydro-3-pyridinyl)methyl]-1-(1-methylethyl)-6-(4-pyridinyl)-1H-pyrazolo[3,4-b]pyridine-4-carboxamideHCID 56597561—

反応手順

The title compound was prepared in the same manner as described in example 9 from 1-(1-methylethyl)-6-(4-pyridinyl)-1H-pyrazolo[3,4-b]pyridine-4-carboxylic acid (403 mg, 1.427 mmol), 3-(aminomethyl)-6-ethyl-4-methyl-2(1H)-pyridinone.TFA (400 mg, 1.427 mmol), HOAT (291 mg, 2.141 mmol), EDC (1094 mg, 5.71 mmol), N-methylmorpholine (0.628 mL, 5.71 mmol), and DMF (6 mL). The final product was collected as a white solid, 232 mg (38%). LCMS E-S (M+H)=432.4. 1H NMR (400 MHz, DMSO-d6) δ ppm 1.14 (t, 3H), 1.56 (d, J=6.57 Hz, 6H), 2.25 (s, 3H), 2.42 (q, J=7.41 Hz, 2H), 4.43 (d, J=4.55 Hz, 2H), 5.29-5.45 (m, 1H), 5.93 (s, 1H), 8.22 (d, J=6.06 Hz, 2H), 8.30 (s, 1H), 8.45 (s, 1H), 8.78 (d, J=5.81 Hz, 2H), 9.01 (t, J=4.55 Hz, 1H), 11.58 (s, 1H).

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US08637509B2
出典データセットuspto-grants-2014_01
ORD IDord-baa8727d001b4f6982f1071e6ee49eba
出典メモuspto-grants-2014_01