5-[(4S)-2,2-Dimethyltetrahydro-2H-pyran-4-yl]-1-[(1S,2S)-2-methyl-1-(5-oxo-4,5-dihydro-1,2,4-oxadiazol-3-yl)cyclopropyl]-1H-indole-2-carboxylic acid

This stereodefined indole-2-carboxylic acid is an advanced orforglipron fragment containing a dimethyltetrahydropyran substituent and an oxadiazolone-bearing methylcyclopropyl group. The carboxyl function supplies the amide-coupling site, while the preassembled heterocycles and stereocenters transfer the required three-dimensional indole fragment into the later molecule.

Its indole nitrogen is already substituted, leaving the carboxyl group as the main late-stage assembly handle. Activation of that acid connects the fragment to a complementary amine-containing core. Keeping the stereodefined ring substituents intact allows the final coupling to unite advanced fragments rather than build those structural elements individually.

Typical Applications

• Orforglipron advanced-fragment coupling: Used as the indole-acid partner in amide formation with the deprotected pyrazolopyridine amine fragment, joining the two advanced portions of the molecule.
• Indole-carboxamide analogue synthesis: Used with alternative amine partners to prepare structurally related amides while retaining the oxadiazolone, cyclopropyl and chiral tetrahydropyran substituents.

Specifications

Specifications describe the standard grade. Tolerance, test method and documentation package are confirmed per order.