4-Amino-6-chlorotoluene-2-sulphonic acid → O-{[(3-chloro-4-methyl-5-sulfophenyl)amino]carbonyl}-L-serine

Participants

Reaction Steps

100 mg (0.38 mmol) of Boc-Ser-OtBu, 86 mg (0.38 mmol) of 5-amino-3-chloro-2-methylbenzenesulfonic acid and 37 mg (0.0127 mmol) of triphosgene were suspended in 1 mL of methylene chloride, and 66 μL (0.76 mmol) of DIEA was added thereto. After stirring the mixture at room temperature overnight, a solvent was removed. Purification was conducted in accordance with the purification process A to obtain a protected form of a title compound. The obtained protected form was dissolved in 2 mL of a trifluoroacetic acid and stirred for 2 hours. After removing a solvent, purification was conducted in accordance with the purification process A to obtain a title compound.

Provenance & Evidence