4-Chlorophenylboronic acid → 5-(4-chloro-phenyl)-N-((1R,2R)-2-hydroxy-cyclohexyl)-6-(3-methyl-isoxazol-5-ylmethoxy)-nicotinamide

反応式

Br[C:2]1[CH:3]=[C:4]([C:9]([OH:11])=O)[CH:5]=[N:6][C:7]=1Cl.[CH3:12][C:13]1[CH:17]=[C:16]([CH2:18][OH:19])[O:15][N:14]=1.[Cl:20][C:21]1[CH:26]=[CH:25][C:24](B(O)O)=[CH:23][CH:22]=1.[NH2:30][C@@H:31]1[CH2:36][CH2:35][CH2:34][CH2:33][C@H:32]1[OH:37]>>[Cl:20][C:21]1[CH:26]=[CH:25][C:24]([C:2]2[C:7]([O:19][CH2:18][C:16]3[O:15][N:14]=[C:13]([CH3:12])[CH:17]=3)=[N:6][CH:5]=[C:4]([CH:3]=2)[C:9]([NH:30][C@@H:31]2[CH2:36][CH2:35][CH2:34][CH2:33][C@H:32]2[OH:37])=[O:11])=[CH:23][CH:22]=1

参加物

反応物 4

HCID 742994-Chlorophenylboronic acid

HCID 2854335-Bromo-6-chloropyridine-3-carboxylic acid

HCID 735777(1R,2R)-2-Aminocyclohexanol

HCID 10820493(3-Methylisoxazol-5-yl)methanol

生成物 1

HCID 119500605-(4-chloro-phenyl)-N-((1R,2R)-2-hydroxy-cyclohexyl)-6-(3-methyl-isoxazol-5-ylmethoxy)-nicotinamide

実験手順

The title compound was synthesized in analogy to Example 75, using 5-bromo-6-chloro-3-pyridinecarboxylic acid, 3-methyl-5-isoxazolemethanol, (4-chloro-phenyl)-boronic acid and (1R,2R)-2-amino-cyclohexanol as starting materials to yield 5-(4-chloro-phenyl)-N-((1R,2R)-2-hydroxy-cyclohexyl)-6-(3-methyl-isoxazol-5-ylmethoxy)-nicotinamide, MS (ISP) 442.4, 444.4 (M+H)+.