A Scalable L‐α‐Glycerophosphorylcholine Synthesis through the Automatic pH‐Controlled (R)‐Glycidol Ring Opening with Phosphorylcholine

Automatic titrator enables the regioselective ring opening of (R)-glycidol in water in the presence of phosphorylcholine, leading to the synthesis of L-α-glycerophosphorylcholine, a commercially available drug, in very high yield. The reaction is triggered by a minimum amount of NaOH and reactants, while the optimal pH is precisely regulated through the automated, controlled addition of phosphorylcholine and (R)-glycidol themselves.

The investigation of epoxide ring opening of (R)-glycidol with phosphorylcholine in water leads to the development of an effective synthesis of L-α-glycerophosphorylcholine (L-α-GPC), a commercially available drug. The precise control of reaction pH with an automatic titrator proves to be crucial for achieving conversions of up to 98% and limiting byproduct formation. Additionally, an effective method for the synthesis of phosphocholine as inner salt is reported for the first time, which is also essential for achieving the described results.

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