Abstract

Racemic or optically active D- or L-α-glycerophosphoryl choline solids are prepared from liquid type racemic or optically active D- or L-α-glycerophosphoryl choline using an organic solvent. The solids are produced at a high yield more easily through phase transformation than an existing method using a difference in solubility in a solvent.

IPC Classes  ?

• C07F 9/113 - Esters of phosphoric acids with unsaturated acyclic alcohols
• C07B 55/00 - RacemisationComplete or partial inversion

Abstract

The present invention is characterized in that racemic or optically active D- or L-α-glycerophosphoryl choline solids are prepared from liquid type racemic or optically active D- or L-α-glycerophosphoryl choline using an organic solvent. The present invention can produce solids at a high yield more easily through phase transformation rather than a method using a difference in solubility in a solvent, which is an existing method.

IPC Classes  ?

• C07F 9/113 - Esters of phosphoric acids with unsaturated acyclic alcohols
• C07B 55/00 - RacemisationComplete or partial inversion

Abstract

A method of preparing racemic or optically active D or L-α-glycerophosphorylcholine in large amounts by subjecting choline phosphate or a salt thereof, and racemic or optically highly pure (S) or (R)-3-halo-1,2-propanediol to a substitution reaction in a medium at high temperature in the presence of an inorganic base which increases the activity of the reaction. The method is cost-effective because of the use of starting materials which are inexpensive compared to those in a conventional method. Moreover, the method is simple and convenient because it is performed via a one-pot reaction without a separate purification process. In addition, it enables a large amount of racemic or optically active D or L-α-glycerophosphorylcholine, or a salt thereof, to be quantitatively produced in a medium without side reactions by using the inorganic base which increases the reaction activity.

IPC Classes  ?

• C07F 9/10 - Phosphatides, e.g. lecithin

Abstract

The present invention is characterized in that racemic or optically active D- or L-α―glycerophosphoryl choline solids are prepared from liquid type racemic or optically active D- or L-α―glycerophosphoryl choline using an organic solvent. The present invention can produce solids at a high yield more easily through phase transformation rather than a method using a difference in solubility in a solvent, which is an existing method.

IPC Classes  ?

• C07F 9/113 - Esters of phosphoric acids with unsaturated acyclic alcohols
• C07B 55/00 - RacemisationComplete or partial inversion
• A61K 31/661 - Phosphorus acids or esters thereof not having P—C bonds, e.g. fosfosal, dichlorvos, malathion
• A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia

Abstract

The present invention relates to a method for preparing racemic or optically active α―glycerophosphoryl choline and, more specifically, to a method for mass-producing racemic or optically active D- or L-α―glycerophosphoryl choline through a substitution reaction of choline phosphate or a salt thereof and racemic or optically pure (S) and (R)-3-halo-1,2-propandiols in the presence of a medium using an inorganic base which increases activity of the reaction at a high temperature. The method for preparing racemic or optically active D- or L-α―glycerophosphoryl choline according to the present invention is economical by using a low-priced starting material compared with the conventional method, provides a convenient preparation procedure by performing a one-pot reaction without a separate purification procedure, and can quantitatively mass-produce racemic or optically active D- or L-α―glycerophosphoryl choline and a salt thereof in the presence of a medium without a side reaction by using an inorganic base which increases activity of the reaction.

IPC Classes  ?

• C07F 9/09 - Esters of phosphoric acids
• C07C 211/63 - Quaternary ammonium compounds having quaternised nitrogen atoms bound to acyclic carbon atoms

Abstract

The present invention relates to a method for preparing Clopidogrel and its derivatives. More particularly, the present invention is a method for preparation of (S)-2-Clopidogrel and its derivatives, which are active inhibitors of platelet aggregation, from an optically active (S)-2-chlorophenylglycine alkyl ester through hydrolysis of racemic 2-chlorophenylglycine alkyl esters using an enzyme. The present invention employs a simple procedure to prepare Clopidogrel and its derivatives.  Because no chiral resolving agents are used except for a small amount of enzyme, the cost of preparation can be reduced. In addition, the present invention is suitable for synthesizing highly optical-active Clopidogrel and its derivatives on a large scale by using optically active (S)-2-chlorophenylglycine alkyl ester obtained in high yield as an intermediate, and is also environmentally friendly since no highly toxic reagents are employed.

IPC Classes  ?

• C07D 495/04 - Ortho-condensed systems