Process for the preparation of N-O-(P-Pivaloyloxybenzenesulfonylamino)-benzoylglycin and for the formulation of the lyophilization containing its mononatrium saltㆍ4 hydrate

摘要

The present invention provides amino acid and the carboxylic acid amide by reaction with a protected glycine derivative 2 Preparation of the amino-benzoyl glycine derivative, and the compound and pivaloyloxy benzene sulfonyl chloride compound and the sulfonyl amide by reacting the carboxyl group is protected N- [O- (P- pivaloyloxymethyl benzenesulfonylamino) benzoyl] geulrisinreul manufactured next, protected N- [O- (P- pivaloyloxymethyl benzenesulfonylamino) benzoyl] geulrisinreul glass was deprotected N- [O- (P- pivaloyloxymethyl benzenesulfonylamino) benzoyl ] geulrisinreul gained, N- [a known method O- (P- pivaloyloxymethyl benzenesulfonylamino) benzoyl] glycine monosodium salt and 4H ₂ O, then the production of this compound in the purified water suspension to produce a clear solution was adjusted to pH 8.0 to 8.5 with sodium ethoxide to N- [O- (P- pivaloyloxymethyl benzenesulfonylamino) benzoyl] glycine monosodium salt and 4H ₂ is characterized by making the freeze-dried product of O.