Sodium Glycinate → {[4-(4-Fluoro-benzyl)-1-hydroxy-3-oxo-6-trifluoromethyl-3,4-dihydro-4,4a-diaza-fluorene-2-carbonyl]-amino}-acetic acid

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Reaction Steps

A mixture of 4-(4-fluoro-benzyl)-1-hydroxy-3-oxo-6-trifluoromethyl-3,4-dihydro-4,4a-diaza-fluorene-2-carboxylic acid methyl ester (100 mg, 0.23 mmol) and sodium glycinate (224 mg, 2.3 mmol) in 2-methoxyethanol (3.3 mL) was microwaved at 150° C. for 1 h and concentrated. Residue was dissolved in water (80 mL) and acidified to pH=3-4 using 1 N HCl solution. Precipitate was collected and rinsed with water. Solid was then dissolved in EtOAc, dried over MgSO4, filtered and concentrated. Crude product was triturated in MeOH (3 mL) and solid was collected and dried in vacuo to provide the title compound 62 mg. ESI (m/z): 476.01 (M−H)−

Provenance & Evidence