Efficient peptide couplings and their use in the synthesis and isolation of a cyclopenta (G) quinazoline trisodium salt
US9458188B2 · kind B2 · utility
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Key dates
| Filing date | Dec 19, 2011 |
| Grant date | Oct 4, 2016 |
| Priority date | — |
| Expiry date | Apr 27, 2032 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07K5/0215
- WIPO fieldOrganic fine chemistry
- WIPO sectorChemistry
Abstract
A new method for the synthesis of L-Glutamyl-γ-D-Glutamic acid and its use in the synthesis of (2R)-((4S)-carboxy-4-(4,N-(((6S)-2-(hydroxymethyl)-4-oxo-3,4,7,8-tetrahydro-3H-cyclopenta[g]quinazolin-6-yl)-N-(prop-2-ynyl)amino)benzamido)butanamido)pentanedioic acid, 1 are provided. Also provided is an efficient method for the isolation and purification of the trisodium salt of the abovementioned acid, 2, in a form suitable for long term storage and use in a parenteral dosing form.
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