5-amino-2,2-dimethylpentanoic acid;hydrochloride

Conditions: temp:0.00; pressure:0.00; stir:; See reaction.notes.procedure_details.

Procedure: A mixture of 1-cyano-4-hydroxy-7-phenoxy-isoquinoline-3-carboxylic acid methyl ester (80 mg, 0.25 mmol) and 5-Amino-2,2-dimethyl-pentanoic acid HCl salt (136 mg, 0.75 mmol) in 0.5 M NaOMe/MeOH (2.5 mL, 5 mmol) was microwaved at 120° C. for 2.5 h. Reaction mixture was diluted with water (100 mL) and acidified by 1 N HCl to pH=3-4. It was extracted with EtOAc. Organic layer was washed with brine, dried over MgSO4, filtered and concentrated. Crude product was purified by silica gel chromatography, eluting with 10-100% EtOAc/hexanes to provide the title compound 17 mg (0.04 mmol) in 16% yield. LC-MS ESI−: 431.94 (M−1)−. was microwaved at 120° C. for 2.5 h Reaction mixture It was extracted with EtOAc Organic layer was washed with brine dried over MgSO4 filtered concentrated Crude product was purified by silica gel chromatography eluting with 10-100% EtOAc/hexanes