4-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole → HCID 59592884, compound
Reaction equation
Cl[C:2]1[N:3]=[C:4]([N:12]2[CH2:17][CH2:16][O:15][CH2:14][CH2:13]2)[C:5]2[S:10][C:9](I)=[CH:8][C:6]=2[N:7]=1.CC1(C)C(C)(C)OB([C:26]2[CH:27]=[N:28][NH:29][CH:30]=2)O1>>[NH:28]1[C:27]2[C:26](=[C:4]([C:2]3[N:3]=[C:4]([N:12]4[CH2:17][CH2:16][O:15][CH2:14][CH2:13]4)[C:5]4[S:10][C:9]([C:26]5[CH:30]=[N:29][NH:28][CH:27]=5)=[CH:8][C:6]=4[N:7]=3)[CH:5]=[CH:6][CH:8]=2)[CH:30]=[N:29]1Participants
3
Procedure
2-Chloro-6-iodo-4-morpholinothieno[3,2-d]pyrimidine 19 (50 mg) was coupled to 4,4,5,5-tetramethyl-2-(1H-pyrazol-4-yl)-1,3,2-dioxaborolane via General Procedure I. The product was purified by reverse phase HPLC to yield 18.1 mg of 203. MS (Q1) 404 (M)+.
Workup
- customThe product was purified by reverse phase HPLC
Sources & evidence
- ORD record
- ord-b53fade766c04ac284a013460d1e9453
- Source dataset
- uspto-grants-2013_05
- Patent number
- US08450315B2
Reaction notes
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