2-(4-Fluoro-phenyl)-7,10-bis-methanesulfonyl-5-methylene-5,6,7,8,9,10-hexahydro-1-oxa-7,10,11-triaza-cycloocta[f]indene-3-carboxylic acid methylamide → 2-(4-Fluoro-phenyl)-7,10-bis-methanesulfonyl-5-methyl-5,6,7,8,9,10-hexahydro-1-oxa-7,10,11-triaza-cycloocta[f]indene-3-carboxylic acid methylamide

Participants

Reaction Steps

To 2-(4-Fluoro-phenyl)-7,10-bis-methanesulfonyl-5-methylene-5,6,7,8,9,10-hexahydro-1-oxa-7,10,11-triaza-cycloocta[f]indene-3-carboxylic acid methylamide (3 mg, 5.74 umol) dissolved in MeOH:EtOAc (1:1 1 mL) was added Dihydroxypalladium (0.5 mg, 2.87 umol). The reaction was fitted with a balloon of H2 and then stirred overnight. The mixture was filtered through a bed of celite and washed with additional MeOH (10 mL) and EtOAc (10 mL) and then concentrated and purified by HPLC CH3CN/H2O/0.1% TFA) to provide 2-(4-Fluoro-phenyl)-7,10-bis-methanesulfonyl-5-methyl-5,6,7,8,9,10-hexahydro-1-oxa-7,10,11-triaza-cycloocta[f]indene-3-carboxylic acid methylamide (140 ug, 3%). MS-ES [M+H]+=525.2.

Provenance & Evidence