2-Ethynylpyrazine → HCID 57775140, compound
Reaction equation
[C:1]([C:3]1[CH:8]=[N:7][CH:6]=[CH:5][N:4]=1)#[CH:2].I[C:10]1[CH:11]=[C:12]([CH:40]=[CH:41][C:42]=1[CH3:43])[C:13]([NH:15][C:16]1[CH:35]=[CH:34][C:19]([CH2:20][N:21]2[CH2:26][CH2:25][N:24](C(OC(C)(C)C)=O)[CH2:23][CH2:22]2)=[C:18]([C:36]([F:39])([F:38])[F:37])[CH:17]=1)=[O:14]>>[CH3:43][C:42]1[CH:10]=[CH:11][C:12]([C:13]([NH:15][C:16]2[CH:35]=[CH:34][C:19]([CH2:20][N:21]3[CH2:22][CH2:23][NH:24][CH2:25][CH2:26]3)=[C:18]([C:36]([F:39])([F:37])[F:38])[CH:17]=2)=[O:14])=[CH:40][C:41]=1[C:2]#[C:1][C:3]1[CH:8]=[N:7][CH:6]=[CH:5][N:4]=1Participants
3
Procedure
The title compound can be synthesized from 2-ethynylpyrazine and tert-butyl 4-(4-(3-iodo-4-methylbenzamido)-2-(trifluoromethyl)benzyl)piperazine-1-carboxylate in a manner similar to that described for Example 1. Following deprotection using saturated MeOH/HCl (g), the product can be obtained as an HCl salt. 2-ethynylpyrazine is prepared from 2-bromopyrazine and ethynyltrimethylsilane according to the 2 steps procedure described in Example 1.
Sources & evidence
- ORD record
- ord-4437aaee6d654b21afc32721707f9fc8
- Source dataset
- uspto-grants-2013_06
- Patent number
- US08461167B2
Reaction notes
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