CS(O[C@:6]1([CH3:18])[CH2:10][CH2:9][CH2:8][N:7]1[C:11]([O:13][C:14]([CH3:17])([CH3:16])[CH3:15])=[O:12])(=O)=O.[C-:19]#[N:20].[Na+]>CN(C=O)C>[C:19]([CH2:18][C@H:6]1[CH2:10][CH2:9][CH2:8][N:7]1[C:11]([O:13][C:14]([CH3:17])([CH3:16])[CH3:15])=[O:12])#[N:20]To a solution of (R)-2-methanesulfonyloxy-methyl-pyrrolidine-1-carboxylic acid, tert-butyl ester (D3) (90 g, 0.32 mol) in DMF (1200 ml) was added sodium cyanide (24 g, 0.49 mol). Heated to 60° C. overnight. Reaction mixture was concentrated and partitioned between water and ether. The organic phase was dried and concentrated to give the title compound (18 g, 30%) (M-Boc) 110.
読み込み中…