Tofogliflozin

China [CN]

Physical State: White to off-white crystalline powder (odorless, bitter taste);

Solubility: Slightly soluble in methanol/ethanol, very slightly soluble in water (solubility ≈ 0.1 mg/mL at pH 7.0), readily soluble in dimethyl sulfoxide (DMSO) and N,N-dimethylformamide (DMF);

Melting Point: Free base: 178~182℃; Hydrate: 154~158℃ (melting range ≤ 4℃ is acceptable);

Optical Rotation: [α]D25 = +108°~+118° (c=1.0, methanol), a key indicator of chiral purity;

Stability: Stable under normal temperature and dry conditions, resistant to light/heat (≤60℃); stable in aqueous solutions (pH 3~7), slowly hydrolyzes under strong acid or alkaline conditions (pH<2 or pH>9) (glucose ring opening);

Crystalline Form: There are two crystalline forms (Form I is the pharmaceutical form, Form II is the metastable form), and strict control of crystalline form uniformity is required in industrial production (affecting dissolution rate and bioavailability).