Back to results
US 2017/0362183 A1Published application
Pyrazolyl carboxylic acid and pyrazolyl urea derivative compounds
AssigneeMerck Sharp & Dohme Corp.
InventorsKristos Adrian Moshos, Valdas Jurkauskas, Yisheng Yang, Youchu Wang
Life of this patent
Estimating the term…
Abstract
Pyrazolyl carboxylic acid and pyrazolyl urea derivatives have been synthesized, which are useful in the manufacture of cephalosporin antibiotic compounds.
Claims20
1-20. (canceled)
A process of making compound (IV) comprising the steps of:
- (a) forming a mixture comprising diphenylphosphoryl azide and compound (XIV):
- (b) adding a solvent comprising water;
- (c) adding NBOC-EDA;
- (d) filtering the mixture and collecting a wet cake comprising crude product;
- and
- (e) obtaining compound (IV):
3 more elements
A process of making compound (XIV):
- comprising the steps of:
- (a) forming a mixture comprising triethylamine and compound (XII):
- (b) adding trityl chloride (ClCPh3) to the mixture of step (a);
- (c) adding an aqueous solution comprising sodium hydroxide;
- (d) adding an aqueous solution comprising hydrochloric acid;
- (e) adding isopropyl acetate and n-heptane;
- and
- (f) obtaining compound (XIV).
5 more elements
The process of claim 18, wherein step (f) further comprises:
- (5) forming a slurry with the wet cake and a mixture of 2:1 (v/v) n-heptane:isopropyl acetate 1.3 volumes of cold ethanol;
- and
- (6) drying the product under reduced pressure with heat.
Dependencies are inferred from the claim text.