Ammonia → HCID 86707943、化合物

反応式

[CH3:1][CH:2]([C:5]1[N:6]([CH2:17][C:18]2[N:23]=[C:22]([C:24](OC)=[O:25])[CH:21]=[CH:20][CH:19]=2)[C:7]2[C:12]([CH:13]=1)=[CH:11][C:10]([O:14][CH3:15])=[C:9]([Cl:16])[CH:8]=2)[CH2:3][CH3:4].O1CCCC1.[NH3:33]>>[CH3:1][CH:2]([C:5]1[N:6]([CH2:17][C:18]2[N:23]=[C:22]([C:24]([NH2:33])=[O:25])[CH:21]=[CH:20][CH:19]=2)[C:7]2[C:12]([CH:13]=1)=[CH:11][C:10]([O:14][CH3:15])=[C:9]([Cl:16])[CH:8]=2)[CH2:3][CH3:4]

参加物

反応物 3

HCID 222Ammonia

HCID 8028Tetrahydrofuran

HCID 67685028HCID 67685028、化合物

生成物 1

HCID 86707943HCID 86707943、化合物

実験手順

To a suspension of methyl 6-[2-(butan-2-yl)-6-chloro-5-methoxyindol-1-ylmethyl]pyridine-2-carboxylate (125 mg) in ammonia (Ca. 7 mol/L methanol solution, 20.1 mL) was added tetrahydrofuran (6.7 mL) at room temperature, followed by stirring for 27 hours. The reaction mixture was concentrated under reduced pressure to obtain the title compound (120 mg). 1H-NMR (CDCl3) δ ppm: 0.86 (3H, t, J=7.5 Hz), 1.25 (3H, d, J=6.9 Hz), 1.45-1.80 (2H, m), 2.65-2.80 (1H, m), 3.93 (3H, s), 5.39 (2H, s), 5.45-5.65 (1H, br), 6.30 (1H, s), 6.65-6.75 (1H, m), 7.11 (1H, s), 7.19 (1H, s), 7.60-7.80 (2H, m), 8.00-8.15 (1H, m).

後処理

concentrationThe reaction mixture was concentrated under reduced pressure

出典と根拠

ORDレコード: ord-46853b343abc4a0d8cc3885139f8af24
出典データセット: uspto-grants-2014_08
DOI: 10.6084/m9.figshare.5104873.v1
特許番号: US08796247B2

反応ノート

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