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Last Updated: December 22, 2024

Claims for Patent: 10,125,149

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Summary for Patent: 10,125,149

Title:	Synthesis of cephalosporin compounds
Abstract:	Provided herein is a method for the synthesis of cephalosporin antibiotic compounds comprising a palladium-catalyzed coupling reaction. Provided herein are methods for the synthesis of cephalosporin compounds of formula (I) employing a palladium-catalyzed alkylation reaction, as well as compositions related to the same. In an aspect, provided herein is a method for preparing a compound of formula (II), or a salt thereof, comprising the step of admixing, e.g., reacting, a compound of formula (III), or a salt thereof, with a nucleophile (Nuc) in the presence of reagents comprising: (a) a palladium source; and (b) a palladium-binding ligand, to form a compound of formula (II), or a salt thereof.
Inventor(s):	Waller; David (Somerville, MA), Gazda; Gregory (Sudbury, MA), Minden; Zachary (Watsonville, CA), Barton; Lisa (Haverhill, MA), Leigh; Clifton (Windham, NH)
Assignee:	Merck Sharp & Dohme Corp. (Rahway, NJ)
Application Number:	15/503,907
Patent Claims:	1. A composition comprising a compound of formula (Va): ##STR00098## and from about 0.01 ppm to about 5 ppm palladium, wherein A.sup..crclbar. is a pharmaceutically acceptable anion selected from chloride, bromide, iodide, sulfate, bisulfate, toluenesulfonate, methanesulfonate, edisylate, maleate, phosphate, ketoglutarate, acetate, trifluoroacetate, and trifluoromethanesulfonate. 2. The composition of claim 1, which comprises from about 0.01 ppm to about 3 ppm palladium. 3. The composition of claim 1, which comprises from about 0.01 ppm to about 2 ppm palladium. 4. The composition of claim 1, which comprises from about 0.01 ppm to about 1 ppm palladium. 5. The composition of claim 1, wherein A.sup..crclbar. is chloride. 6. The composition of claim 1, wherein A.sup..crclbar. is bisulfate. 7. The composition of claim 1, wherein A.sup..crclbar. is acetate. 8. The composition of claim 1, wherein A.sup..crclbar. is trifluoroacetate. 9. A composition comprising a compound of formula (VII): ##STR00099## and from about 0.01 ppm to about 5 ppm palladium. 10. The composition of claim 9, which comprises from about 0.01 ppm to about 3 ppm palladium. 11. The composition of claim 9, which comprises from about 0.01 ppm to about 2 ppm palladium. 12. The composition of claim 9, which comprises from about 0.01 ppm to about 1 ppm palladium. 13. A composition comprising a compound of formula (VII): ##STR00100## and from about 0.01 ppm to about 1 ppm palladium.

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