2-(Pyridin-3-yloxy)ethan-1-ol → PRX933 hydrochloride
Reaktionsgleichung
[N:1]1[CH:6]=[CH:5][CH:4]=[C:3]([O:7][CH2:8][CH2:9][OH:10])[CH:2]=1.[Cl:11][C:12]1[C:13]([N:18]2[CH2:23][CH2:22][N:21](C(OC(C)(C)C)=O)[CH2:20][C@H:19]2[CH3:31])=[N:14][CH:15]=[CH:16][N:17]=1>>[ClH:11].[CH3:31][C@@H:19]1[CH2:20][NH:21][CH2:22][CH2:23][N:18]1[C:13]1[C:12]([O:10][CH2:9][CH2:8][O:7][C:3]2[CH:2]=[N:1][CH:6]=[CH:5][CH:4]=2)=[N:17][CH:16]=[CH:15][N:14]=1Komponenten
3
Versuchsvorschrift
The title compound was prepared starting from 2-(3-pyridyloxy)ethanol (from Example 150, Step 1) and 3-chloro-2-[4-tert-butoxycarbonyl-(2R)-methyl-1-piperazinyl]pyrazine (from Example 172, Step 2). The pure free base was precipitated as its hydrochloride salt with HCl/ether to give the title compound as white crystals: yield 31%; mp 180-183° C.; HRMS m/z calcd for C16H21N5O2 (M)+ 315.1695, found 315.1689. Anal. (C16H21N5O2.1.33HCl) C, H, N.
Aufarbeitung
- customThe title compound was prepared
- customThe pure free base was precipitated as its hydrochloride salt with HCl/ether