Pyridine → HCID 145857654, compound

Participants

Reaction Steps

To a solution of {[4-(2′-amino-6′-methyl-biphenyl-3-sulfonyl)-5-methylsulfanyl-thiophen-2-yl]-imino-methyl}-carbamic acid tert-butyl ester (60 mg, 0.116 mmol), as prepared according to the procedure of step c of Example 25, and pyridine (10 mg, 0.128 mmol) in DCM (1.1 mL) was added 4-nitrophenyl chloroformate (23 mg, 0.116 mmol), and stirred at ambient temperature for 4 h. To the above mixture was added a solution of 4-(2-trityl-2H-tetrazol-5-yl)-butylamine (65 mg, 0.151 mmol) in DCM (0.65 mL), and stirred for 48 h. The mixture was concentrated and purified on a preparative TLC plate (1000 μm), developing with EtOAc/DCM (5 and 20%) to give the title compound (15 mg, 14% yield) as a yellow solid.

Provenance & Evidence