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US 8,134,026 B2Granted
Process for the preparation of Cilastatin and sodium salt
AssigneeOrchid Chemicals & Pharmaceuticals Limited
InventorsGanapathy Panchapakesan, Nagappan Arumugam, Pandi Suresh Pandian, Gollapalli Venkateswara Rao, Subramaniam Ganesan
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Abstract
The present invention relates to an improved process for the preparation of Cilastatin Sodium of formula (I). The present invention also provides an isolation technique for Cilastatin acid from the reaction mixture.
Claims4
An improved process for the preparation of Cilastatin Acid of formula (I),
- the process comprises the steps of:
- i) condensing 7-chloro-2-[[(1S)-2,2-dimethylcyclopropane]carboxamide]-2-heptenoic acid of formula (II)
- with L-Cysteine in the presence of a base and an alcoholic solvent or an aqueous alcoholic solvent;
- ii) optionally removing inorganic salts by filtration and concentrating filtrate;
- iii) optionally adding water;
- iv) adjusting pH to 2.0 to 4.0;
- v) extracting the Cilastatin acid into C4-C8 alcohol selected from the group consisting of n-butanol and cyclohexanol;
- and
- vi) isolating Cilastatin acid.
6 more elements
Dependencies are inferred from the claim text.