Processes for the preparation and purification of gabapentin enacarbil

摘要

Gabapentin enacarbil was prepared and purified from intermediates such as 1-haloalkyl carbamate or carbonate and diacid acetal skeleton. For example, a 1-haloalkyl carbonate or carbamate was prepared by combining a C₁ to C₁₀ alcohol or C₁ to C₁₀ primary amine, a solvent selected from the group consisting of: acetonitrile, C₃ to C₇ ketone, C₅ to C₁₀ ether, C₂ to C₇ ester, C₅ to C₁₀ hydrocarbon and a combination thereof; a 1-haloalkyl haloformate of the following formula:; wherein each X is independently selected from Br, I, or Cl; R₁ is alkyl or H; and a C₆ to C₂₁ tertiary amine.