1-Fluoro-3-iodobenzene → 2-{4-[3-(3-Fluorophenyl)prop-2-ynylidene]piperidin-1-yl}-6-methylnicotinonitrile
반응식
C[Si](C)(C)C#CC=C1CC[NH:9][CH2:8]C1.[F:14][C:15]1[CH:20]=[CH:19][CH:18]=[C:17](I)[CH:16]=1.[CH3:22][C:23]1[N:28]=[C:27]([N:29]2[CH2:34][CH2:33][C:32](=[CH:35][C:36]#[CH:37])[CH2:31][CH2:30]2)[C:26]([N+]([O-])=O)=[CH:25][CH:24]=1>>[F:14][C:15]1[CH:16]=[C:17]([C:37]#[C:36][CH:35]=[C:32]2[CH2:33][CH2:34][N:29]([C:27]3[N:28]=[C:23]([CH3:22])[CH:24]=[CH:25][C:26]=3[C:8]#[N:9])[CH2:30][CH2:31]2)[CH:18]=[CH:19][CH:20]=1참가 물질
4
실험 절차
The title compound was prepared in the same way as the Compound of Example 274 but replacing 1-bromo-3,5-difluorobenzene with 1-fluoro-3-iodobenzene and Compound 274c with Compound 284a. The residue coming from the work-up procedure was purified by preparative RP LC-MS chromatography, using MS-C18 XTerra column 30×50 mm eluting with ammonium bicarbonate 20 mM pH 8 buffer-acetonitrile gradient affording the title compound as a colourless oil. Yield: 20.4%