1,8-Diazabicyclo(5.4.0)undec-7-ene → 3-{[7-Cyano-7-(2-fluoro-phenoxy)-4-hydroxy-isoquinoline-3-carbonyl]amino}-2-cyclopropyl-propionic acid tert-butyl ester

Participants

Reaction Conditions

Reaction Steps

A mixture of 3-amino-2-cyclopropyl-propionic acid tert-butyl ester (15 mg), 1-cyano-7-(2-fluoro-phenoxy)-4-hydroxy-isoquinoline-3-carboxylic acid methyl ester (11 mg) and DBU (0.0074 mL) in DMA (0.5 mL) was heated in an oil bath (150° C.) for 1 h. The reaction mixture was then partitioned between EtOAc and diluted HCl solution, EtOAc phase was separated and washed with water, diluted NaCl solution and dried over anhydrous sodium sulfate solution, filtered, concentrated and silica gel column purified to give desired product (10 mg). LC-MS ESI+: 492 (M+1)+.

Provenance & Evidence