反応式
[NH2:1][CH:2]1[CH2:7][CH2:6][N:5]([CH2:8][C@H:9]2[C:13]3=[C:14]([F:22])[CH:15]=[N:16][C:17]4[CH:18]=[CH:19][C:20](=[O:21])[N:11]([C:12]=43)[CH2:10]2)[CH2:4][CH2:3]1.[Cl:23][C:24]1[C:33]([CH:34]=O)=[N:32][C:31]2[NH:30][C:29](=[O:36])[CH2:28][O:27][C:26]=2[CH:25]=1.C(O[BH-](OC(=O)C)OC(=O)C)(=O)C.C(=O)(O)[O-].[Na+]>ClCCl.CO>[ClH:23].[Cl:23][C:24]1[C:33]([CH2:34][NH:1][CH:2]2[CH2:7][CH2:6][N:5]([CH2:8][C@H:9]3[C:13]4=[C:14]([F:22])[CH:15]=[N:16][C:17]5[CH:18]=[CH:19][C:20](=[O:21])[N:11]([C:12]=54)[CH2:10]3)[CH2:4][CH2:3]2)=[N:32][C:31]2[NH:30][C:29](=[O:36])[CH2:28][O:27][C:26]=2[CH:25]=1参加物
7
反応物 4
生成物 1
試薬・触媒・溶媒 2
実験手順
A mixture of (4R)-4-[(4-amino-1-piperidinyl)methyl]-3-fluoro-4,5-dihydro-7H-pyrrolo[3,2,1-de]-1,5-naphthyridin-7-one Enantiomer 1 (50 mg, 016 mmol) and 7-chloro-3-oxo-3,4-dihydro-2H-pyrido[3,2-b][1,4]oxazine-6-carboxaldehyde (for a synthesis see WO2003064421, Example 15(c) (33 mg, 0.16 mmol) in anhydrous dichloromethane (1.5 mL) and anhydrous methanol (0.1 mL) was treated with triacetoxyborohydride (105 mg, 0.49 mmol). After 16 hours, an aqueous solution of sodium bicarbonate was added. The free base of the title compound came out of solution and was isolated by filtration, washed with water and dried in vacuo (50 mg, 60%).
出典と根拠
- ORDレコード
- ord-227e0690a15443a9b364ea0c110396ff
- 出典データセット
- uspto-grants-2010_06
- 特許番号
- US07732461B2
関連ノート
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