Methanesulfonyl chloride → HCID 86679506, compound

Participants

Reaction Steps

To a solution of crude methyl 2-(3-amino-4-(cyclopropylmethoxy)phenyl)acetate (theoric 4.74 mmol) in pyridine (50 ml), methanesulfonyl chloride (0.406 ml, 5.10 mmol) was added, and the mixture was reacted for 3 hours at RT. The solvent was evaporated to dryness, and the residue was partitioned between EtOAc and HCl 1N; the aqueous phase was extracted with EtOAc (3×), and the combined organic layers were dried over Na2SO4. The solvent was removed under vacuum affording methyl 2-(4-(cyclopropylmethoxy)-3-(methylsulfonamido)phenyl)acetate (1.4 g, 4.47 mmol, 94.3% yield over 3 steps, MS/ESI+ 313.9 [MH]+). This intermediate was used without any additional purification.

Provenance & Evidence