反応式
C([BH3-])#N.[Na+].[NH2:5][C@@H:6]([CH2:11][C:12]1[CH:17]=[CH:16][CH:15]=[CH:14][CH:13]=1)[C:7]([O:9][CH3:10])=[O:8].O=[CH:19][C@H:20]([NH:22]C(=O)OC(C)(C)C)[CH3:21].[ClH:30].FC(F)(F)C(O)=O.Cl.O1CCOCC1.[CH:45]1[C:54]2[C:49](=[CH:50][C:51]([S:55]([Cl:58])(=[O:57])=[O:56])=[CH:52][CH:53]=2)[CH:48]=[CH:47][N:46]=1>CO.C(O)(=O)C>[ClH:58].[ClH:30].[CH:45]1[C:54]2[C:49](=[CH:50][C:51]([S:55]([NH:22][C@H:20]([CH3:21])[CH2:19][NH:5][C@@H:6]([CH2:11][C:12]3[CH:17]=[CH:16][CH:15]=[CH:14][CH:13]=3)[C:7]([O:9][CH3:10])=[O:8])(=[O:57])=[O:56])=[CH:52][CH:53]=2)[CH:48]=[CH:47][N:46]=1参加物
10
反応物 7
生成物 1
試薬・触媒・溶媒 2
実験手順
Sodium cyanoborohydride (1.1 g) and acetic acid (0.75 mL) were added to a mixture of methyl (S)-2-amino-3-phenylpropanoate (2.72 g) and (R)-tert-butyl 1-oxopropan-2-ylcarbamate (1.97 g) in methanol to perform reductive amination (2.37 g, 46%). Next, deprotection and conversion to hydrochloride were performed (1.0 g, 45%) using trifluoroacetic acid and a 4 M hydrochloric acid-1,4-dioxane solution, followed by subjecting to condensation with isoquinoline-6-sulfonyl chloride prepared in Reference Example 1 (1.04 g, 75%). 28 mg of the title compound was obtained as a white solid (29%) with reference to the method of Step 3 of Example 1 using 80 mg of the obtained product.
出典と根拠
- ORDレコード
- ord-7fa4342ce9dd47479ff1ba03801a5dde
- 出典データセット
- uspto-grants-2014_11
- 特許番号
- US08883792B2
関連ノート
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