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US 10,941,161 B2Granted
Intermediates in the synthesis of cephalosporin compounds
AssigneeMerck Sharp & Dohme Corp.
InventorsKristos Adrian Moshos, Valdas Jurkauskas, Giovanni Fogliato, Manuel Scanu, You Seok Hwang
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Abstract
Described herein are crystalline forms of a compound of formula (III′), including toluene solvates of TATD-CLE, as well as processes for the preparation thereof and use thereof in the preparation of cephalosporin compounds such as ceftolozane.
Claims20
A process for making a compound of formula (VI):
- comprising admixing a crystalline form of a compound of formula (III):
- wherein PMB is 4-methoxybenzyl and wherein the crystalline form of a compound of formula (III) is a solvate of an aromatic solvent,
- with a compound of formula (IV):
- to give a compound of formula (V):
- and contacting the compound of the formula (V) with a strong acid, followed by crystallization with sulfuric acid to provide the compound of formula (VI).
2 more elements
A process for making a compound of formula (VI):
- comprising admixing a crystalline form of a compound of formula (III′):
- wherein
- X is Cl, Br, or I;
- and
- R1 and R2 are each independently an oxygen protecting group, and wherein the crystalline form of a compound of formula (III) is a solvate of an aromatic solvent, with a compound of formula (IV′):
- wherein
- R5 and R6 are each independently a nitrogen protecting group;
- to give a compound of formula (V″):
- wherein A⊖ is a pharmaceutically acceptable anion;
- and contacting the compound of the formula (V′) with a strong acid, followed by crystallization with sulfuric acid to provide the compound of formula (VI).
7 more elements
Dependencies are inferred from the claim text.