HCID 86683571、化合物 → 1-(6-(4-(1-aminocyclobutyl)phenyl)-7-phenyl-2,3-dihydro-1H-pyrido[2,3-b][1,4]oxazin-1-yl)ethanone

HRID 1509143ノート

反応式

HRID 1509143 の反応式
[C:1]([N:4]1[CH2:9][CH2:8][O:7][C:6]2[N:10]=[C:11]([C:20]3[CH:25]=[CH:24][C:23]([C:26]4([NH:30]C(=O)OC(C)(C)C)[CH2:29][CH2:28][CH2:27]4)=[CH:22][CH:21]=3)[C:12]([C:14]3[CH:19]=[CH:18][CH:17]=[CH:16][CH:15]=3)=[CH:13][C:5]1=2)(=[O:3])[CH3:2]>Cl.CCOCC>[NH2:30][C:26]1([C:23]2[CH:22]=[CH:21][C:20]([C:11]3[C:12]([C:14]4[CH:15]=[CH:16][CH:17]=[CH:18][CH:19]=4)=[CH:13][C:5]4[N:4]([C:1](=[O:3])[CH3:2])[CH2:9][CH2:8][O:7][C:6]=4[N:10]=3)=[CH:25][CH:24]=2)[CH2:27][CH2:28][CH2:29]1

参加物

4

反応物 1

HCID 86683571HCID 86683571、化合物

生成物 1

HCID 532620521-(6-(4-(1-aminocyclobutyl)phenyl)-7-phenyl-2,3-dihydro-1H-pyrido[2,3-b][1,4]oxazin-1-yl)ethanone収率 131.4%

試薬・触媒・溶媒 2

HCID 313Hydrochloric Acid溶媒HCID 3283Diethyl Ether溶媒

実験手順

Tert-butyl (1-(4-(1-acetyl-7-phenyl-2,3-dihydro-1H-pyrido[2,3-b][1,4]oxazin-6-yl)phenyl)cyclobutyl)carbamate (20 mg, 0.04 mmol) was dissolved in 2M HCl in Et2O (1 ml). The resulting mixture was stirred overnight at room temperature and evaporated under reduced pressure. The deprotected compound was taken back twice into diethyl ether. The remaining solvent was removed under reduced pressure and dried to afford the title compound (21 mg, quantitative). LCMS (Method A): RT=3.87 min, M-16=383. 1H NMR (500 MHz, MeOD): 8.70 (1H, br s), 7.44-7.43 (4H,m), 7.30-7.28 (3H, m), 7.21-7.19 (2H, m), 4.63 (2H, t), 4.11 (2H, t), 2.75-2.70 (2H, m), 2.56-2.50 (2H, m), 2.42 (3H, s), 2.24-2.15 (1H, m), 1.97-1.88 (1H, m).

後処理

  1. customevaporated under reduced pressure
  2. customThe remaining solvent was removed under reduced pressure
  3. customdried

出典と根拠

ORDレコード
ord-30825ec25b4546779e12d0b258977484
出典データセット
uspto-grants-2015_12
特許番号
US09221838B2

反応ノート

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