反应方程式
CN(C(ON1N=NC2C=CC=NC1=2)=[N+](C)C)C.F[P-](F)(F)(F)(F)F.[Br:25][C:26]1[C:27]([OH:35])=[N:28][CH:29]=[C:30]([CH:34]=1)[C:31]([OH:33])=O.CCN(C(C)C)C(C)C.Cl.[F:46][C:47]1[C:48]([C@H:53]([C:55]2[CH:60]=[CH:59][C:58]([C:61]([F:64])([F:63])[F:62])=[CH:57][CH:56]=2)[NH2:54])=[N:49][CH:50]=[CH:51][CH:52]=1.Cl.FC(F)(F)C1C=CC([C@@H](C2C(C(F)(F)F)=CC=CN=2)N)=CC=1>C(Cl)Cl>[Br:25][C:26]1[C:27](=[O:35])[NH:28][CH:29]=[C:30]([C:31]([NH:54][C@H:53]([C:48]2[C:47]([F:46])=[CH:52][CH:51]=[CH:50][N:49]=2)[C:55]2[CH:60]=[CH:59][C:58]([C:61]([F:62])([F:63])[F:64])=[CH:57][CH:56]=2)=[O:33])[CH:34]=1参与物
7
反应物 5
HCID 81531N,N-二异丙基乙胺
HCID 9886157Methanaminium, N-((dimethylamino)(3H-1,2,3-triazolo(4,5-b)pyridin-3-yloxy)methylene)-N-methyl-, hexafluorophosphate(1-) (1:1)
HCID 71144279(S)-(3-Fluoropyridin-2-yl)(4-(trifluoromethyl)phenyl)methanamine Hydrochloride
HCID 86687962(S)-(4-(Trifluoromethyl)phenyl)(3-(trifluoromethyl)pyridin-2-yl)methanamine Hydrochloride
HCID 178524767HCID 178524767，化合物产物 1
试剂、催化剂与溶剂 1
实验过程
To a solution of HATU (0.332 g, 0.874 mmol) in DCM (2 mL) was added 5-bromo-6-hydroxynicotinic acid (0.191 g, 0.874 mmol) and DIPEA (0.406 mL, 2.331 mmol). The resulting mixture was then stirred at rt for 5 min, then (S)-(3-fluoropyridin-2-yl)(4-(trifluoromethyl)phenyl)methanamine hydrochloride (Intermediate 2) (0.200 g, 0.583 mmol) was added. The mixture was then stirred at rt overnight. The mixture was purified by silica gel column chromatography using an ISCO instrument (0%-100% EtOAc/hexane) to give the title compound as a brown oil.
后处理
- stirringThe mixture was then stirred at rt overnight
- customThe mixture was purified by silica gel column chromatography
来源与证据
- ORD记录
- ord-cbbbad2a287d43ed990895938d9c2c66
- 来源数据集
- uspto-grants-2015_08
- 专利号
- US09096527B2
关联笔记
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