5-[(S)-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

Its molecular formula is C₂₂H₂₅N₃O₅, with a molecular weight of 411.45 g/mol. The compound features two fixed chiral centers: (S)-configured tetrahydro-2H-pyran-4-yl and (1S,2S)-configured disubstituted cyclopropyl, integrated with indole mother nucleus, 5-oxo-4,5-dihydro-1,2,4-oxadiazole pharmacophore and 2,2-dimethyltetrahydropyran lipophilic group, which endows it with balanced structure-activity relationship and pharmacokinetic potential.

Physically, it appears as an off-white to light yellow crystalline powder at room temperature, soluble in polar organic solvents such as methanol and dichloromethane but poorly soluble in water. It is stable under dry, dark and neutral conditions, decomposes easily in strong acid or alkali environments, and has a melting point of 178-182℃ with slight decomposition.

As a critical chiral intermediate, DTIOC is the key building block for the synthesis of Orforglipron (a promising oral small-molecule GLP-1 receptor agonist) and is mainly used in the R&D and pilot-scale synthesis of drugs targeting malignant tumors, chronic inflammatory diseases and central nervous system disorders. For pharmaceutical intermediate grade, its key quality specifications include HPLC purity ≥98.5%, chiral purity (ee) ≥98.0%, water content ≤0.3% and total heavy metals ≤10 ppm.

It should be stored in vacuum-sealed, moisture-proof and light-proof containers at 2-8℃ for long-term storage. Operation should be carried out in a fume hood with full protective gear to avoid skin contact and powder inhalation. It is only for pharmaceutical R&D and intermediate synthesis, not for clinical use.