Patent classifications
C07C227/34
Method for resolution of baclofen salts
The invention relates to the field of resolution of chiral compounds existing in the form of two optical antipodes (enantiomers), such as Baclofen. More particularly, the invention relates to the production of the pure enantiomer (R)(−) Baclofen, of chemical nomenclature (R)-4-amino-3-(4-chlorophenyl)-butanoic acid, and the hydrogen maleate salt thereof. More specifically, the invention relates to the resolution of hydrogen maleate salts of racemic Baclofen by preferential crystallisation and particularly by the AS3PC method (auto-seeded and programmed polythermal preferential crystallisation).
Method for resolution of baclofen salts
The invention relates to the field of resolution of chiral compounds existing in the form of two optical antipodes (enantiomers), such as Baclofen. More particularly, the invention relates to the production of the pure enantiomer (R)(−) Baclofen, of chemical nomenclature (R)-4-amino-3-(4-chlorophenyl)-butanoic acid, and the hydrogen maleate salt thereof. More specifically, the invention relates to the resolution of hydrogen maleate salts of racemic Baclofen by preferential crystallisation and particularly by the AS3PC method (auto-seeded and programmed polythermal preferential crystallisation).
Method for resolution of baclofen salts
The invention relates to the field of resolution of chiral compounds existing in the form of two optical antipodes (enantiomers), such as Baclofen. More particularly, the invention relates to the production of the pure enantiomer (R)(−) Baclofen, of chemical nomenclature (R)-4-amino-3-(4-chlorophenyl)-butanoic acid, and the hydrogen maleate salt thereof. More specifically, the invention relates to the resolution of hydrogen maleate salts of racemic Baclofen by preferential crystallisation and particularly by the AS3PC method (auto-seeded and programmed polythermal preferential crystallisation).
METHOD FOR PRODUCING 2-OCTYLGLYCINE ESTER HAVING OPTICAL ACTIVITY
A method for producing a 2-octylglycine ester having optical activity from a racemic 2-octyl-DL-glycine ester and, more particularly, to a method for producing a 2-octyl-L-glycine ester or a 2-octyl-D-glycine ester by using a chiral mandelic acid as an optical resolution agent.
METHOD FOR PRODUCING 2-OCTYLGLYCINE ESTER HAVING OPTICAL ACTIVITY
A method for producing a 2-octylglycine ester having optical activity from a racemic 2-octyl-DL-glycine ester and, more particularly, to a method for producing a 2-octyl-L-glycine ester or a 2-octyl-D-glycine ester by using a chiral mandelic acid as an optical resolution agent.
METHOD FOR PRODUCING 2-OCTYLGLYCINE ESTER HAVING OPTICAL ACTIVITY
A method for producing a 2-octylglycine ester having optical activity from a racemic 2-octyl-DL-glycine ester and, more particularly, to a method for producing a 2-octyl-L-glycine ester or a 2-octyl-D-glycine ester by using a chiral mandelic acid as an optical resolution agent.
A CHIRAL RESOLUTION METHOD MIMICKING MAGNETIC BENEFICIATION AND THE MAGNETIC NANO-INHIBITORS FOR SELECTIVE ENRICHMENT
A core-shell nanocomposite is formed by co-assembly of an amphiphilic polymer and hydrophobically modified magnetic nanoparticles, with its core being a hydrophobically modified magnetic nanomaterial and its shell being the amphiphilic polymer, wherein hydrophilic segments in the amphiphilic polymer are located at an outermost layer of the shell. The above composite can be used as additives in the crystallization of conglomerates and obtain optically pure crystals of both enantiomers in a single process. The key thereof is that the composite is used to enrich molecules with the same configuration while inhibit the crystallization of the other enantiomer in a supersaturated solution of conglomerates, such that a non-magnetic crystal and a magnetic crystal (which are enantiomers of each other) are generated in a unit operation. Optically pure crystals of both enantiomers with over 90 ee % can be obtained by one-time crystallization, and the total yield can be as high as 40%.
A CHIRAL RESOLUTION METHOD MIMICKING MAGNETIC BENEFICIATION AND THE MAGNETIC NANO-INHIBITORS FOR SELECTIVE ENRICHMENT
A core-shell nanocomposite is formed by co-assembly of an amphiphilic polymer and hydrophobically modified magnetic nanoparticles, with its core being a hydrophobically modified magnetic nanomaterial and its shell being the amphiphilic polymer, wherein hydrophilic segments in the amphiphilic polymer are located at an outermost layer of the shell. The above composite can be used as additives in the crystallization of conglomerates and obtain optically pure crystals of both enantiomers in a single process. The key thereof is that the composite is used to enrich molecules with the same configuration while inhibit the crystallization of the other enantiomer in a supersaturated solution of conglomerates, such that a non-magnetic crystal and a magnetic crystal (which are enantiomers of each other) are generated in a unit operation. Optically pure crystals of both enantiomers with over 90 ee % can be obtained by one-time crystallization, and the total yield can be as high as 40%.
Process for electrochemical separation of enantiomers of an amino acid from a racemic mixture
The present disclosure relates to a process for separation of enantiomers of the amino acid from a racemic mixture. The process comprises electrolyzing the first electrolyte having 1 molar solution of lithium perchlorate and 0.01 molar solution of racemic mixture of amino acid in an electrochemical cell containing a working electrode having polycrystalline metal surface configured to adsorb L-enantiomer of amino acid using a saw-tooth current. Further, the polarity of the saw-tooth current is reversed to de-adsorb the L-enantiomer of amino acid from the working electrode into the second electrolyte re-filled in the cell. The process of the present disclosure to separate enantiomer of amino acid from a racemic mixture is simple and economical.
Process for electrochemical separation of enantiomers of an amino acid from a racemic mixture
The present disclosure relates to a process for separation of enantiomers of the amino acid from a racemic mixture. The process comprises electrolyzing the first electrolyte having 1 molar solution of lithium perchlorate and 0.01 molar solution of racemic mixture of amino acid in an electrochemical cell containing a working electrode having polycrystalline metal surface configured to adsorb L-enantiomer of amino acid using a saw-tooth current. Further, the polarity of the saw-tooth current is reversed to de-adsorb the L-enantiomer of amino acid from the working electrode into the second electrolyte re-filled in the cell. The process of the present disclosure to separate enantiomer of amino acid from a racemic mixture is simple and economical.