3-氨基-2,2-二甲基丙酸

反应条件: temp:0.00; pressure:0.00; stir:; See reaction.notes.procedure_details.

实验步骤: A mixture of 1-cyano-4-hydroxy-7-phenoxy-isoquinoline-3-carboxylic acid methyl ester (82 mg, 0.26 mmol) and 3-amino-2,2-dimethyl-propionic acid (90 mg, 0.77 mmol) (ChemBridge) in 0.5 M NaOMe/MeOH (1.0 mL, 0.5 mmol) was microwaved at 120° C. for 40 min. Reaction mixture was concentrated and the residue was dissolved in water (70 mL). It was acidified by 1 N HCl to pH=3-4. Precipitate was collected, rinsed with water and dried. Crude product was triturated with MeOH (2 mL). solid was collected and dried to provide the title compound 54.4 mg (0.13 mmol) in 51% yield. LC-MS ESI−: 404.03 (M−1)−. was microwaved at 120° C. for 40 min Reaction mixture was concentrated the residue was dissolved in water (70 mL) Precipitate was collected rinsed with water dried Crude product was triturated with MeOH (2 mL) solid was collected dried

反应条件: temp:0.00; pressure:0.00; stir:; See reaction.notes.procedure_details.

实验步骤: A mixture of 4-hydroxy-7-phenoxy-isoquinoline-3-carboxylic acid methyl ester (68 mg, 0.23 mmol) and 3-amino-2,2-dimethyl-propionic acid (81 mg, 0.69 mmol) (ChemBridge) in 0.5 N NaOMe in MeOH solution (0.92 mL, 0.46 mmol) was microwaved at 120° C. for 1 h. Reaction mixture was diluted with water (50 mL) and acidified by 1 N HCl solution to pH=3-4. Precipitate was collected and rinsed with water and dried in vacuo to provide the title compound (71 mg, 0.19 mmol) as an off-white solid in 81% yield. LC-MS ESI−: 379.04 (M−1)−. was microwaved at 120° C. for 1 h Reaction mixture Precipitate was collected rinsed with water dried in vacuo