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US 11,623,943 B2Granted
Method for producing lacosamide and intermediate thereof
AssigneeApi Corporation
InventorMasaki Nagahama
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Abstract
The present invention provides a method of industrially and safely producing lacosamide high in diastereomeric excess at a high yield and a low cost. Adopting a particular isomerization-crystallization condition makes it possible to a method of industrially and safely producing lacosamide high in diastereomeric excess at a high yield and a low cost. Additionally, an intermediate efficacious for producing lacosamide is provided.
Claims4
A crystal of a salt of R-configuration of
- N-benzyl-2-amino-3-methoxypropionamide and
- N-acetylamino acid, wherein
- the N-acetylamino acid is N-acetyl-D-Leucine;
- and
- the salt of R-configuration of
- N-benzyl-2-amino-3-methoxypropionamide and
- N-acetylamino acid
- has a powder X-ray diffraction measuring pattern using a CuKα ray exhibiting peaks at diffraction angles (2θ±0.2°)=6.3°, 15.8°, 18.1°, 23.4° and 25.2°.
5 more elements
A crystal of a salt of R-configuration of
- N-benzyl-2-amino-3-methoxypropionamide and
- N-acetylamino acid, wherein
- the N-acetylamino acid is N-acetyl-D-Valine;
- and
- the salt of R-configuration of
- N-benzyl-2-amino-3-methoxypropionamide and
- N-acetylamino acid
- has a powder X-ray diffraction measuring pattern using a CuKα ray exhibiting peaks at diffraction angles (2θ±0.2°)=7°, 14.8°, 18.7°, 21.9° and 24.6°.
5 more elements
A crystal of a salt of R-configuration of
- N-benzyl-2-amino-3-methoxypropionamide and
- N-formylamino acid, wherein
- the N-formylamino acid is N-formyl-L-Leucine;
- and
- the salt of R-configuration of
- N-benzyl-2-amino-3-methoxypropionamide and
- N-formylamino acid
- has a powder X-ray diffraction measuring pattern using a CuKα ray exhibiting peaks at diffraction angles (2θ±0.2°)=4.9°, 9.4°, 12.4°, 18.7°, 24.9° and 26.9°.
5 more elements
A crystal of a salt of R-configuration of
- N-benzyl-2-amino-3-methoxypropionamide and
- N-formylamino acid, wherein
- the N-formylamino acid is N-formyl-L-Alanine;
- and
- the salt of R-configuration of
- N-benzyl-2-amino-3-methoxypropionamide and
- N-formylamino acid
- has a powder X-ray diffraction measuring pattern using a CuKα ray exhibiting peaks at diffraction angles (2θ±0.2°)=9.9°, 12°, 17.8°, 19.8°, 22.4°, 24° and 25.3°.
5 more elements
Dependencies are inferred from the claim text.