C07C255/59

Processes and intermediates for making sweet taste enhancers

The present invention includes methods/processes and intermediates for preparing compounds having structural Formula (XI): ##STR00001##
wherein Y is C.sub.1-C.sub.12 alkylene or C.sub.1-C.sub.12 alkenylene; and R.sup.8 and R.sup.12 are independently C.sub.1-C.sub.12 alkyl.

Processes and intermediates for making sweet taste enhancers

The present invention includes methods/processes and intermediates for preparing compounds having structural Formula (XI): ##STR00001##
wherein Y is C.sub.1-C.sub.12 alkylene or C.sub.1-C.sub.12 alkenylene; and R.sup.8 and R.sup.12 are independently C.sub.1-C.sub.12 alkyl.

CATECHOL O-METHYLTRANSFERASE ACTIVITY INHIBITING COMPOUNDS

Compounds of formula (I), wherein R.sub.1 is as defined in the claims, exhibit COMT enzyme inhibiting activity and are thus useful as COMT inhibitors. Methods of treatment and pharmaceutical dosage forms are also disclosed.

CATECHOL O-METHYLTRANSFERASE ACTIVITY INHIBITING COMPOUNDS

Compounds of formula (I), wherein R.sub.1 is as defined in the claims, exhibit COMT enzyme inhibiting activity and are thus useful as COMT inhibitors. Methods of treatment and pharmaceutical dosage forms are also disclosed.

OPTICAL ELEMENT, MATERIAL, OPTICAL APPARATUS AND COMPOUND
20200012014 · 2020-01-09 ·

The triarylamine compound is represented by the following general formula (1), and the material, the optical element, and the optical apparatus each include a polymerized product (cured product) of the triarylamine compound.

##STR00001##

(In the general formula (1), R.sup.1 and R.sup.2 are each independently selected from a substituted or unsubstituted alkyl group having 1 to 10 carbon atoms, and a substituted or unsubstituted alkylene group having 1 to 8 carbon atoms, the alkylene group having a polymerizable functional group, and R.sup.3 to R.sup.12 are each independently selected from a hydrogen atom, a cyano group, a trifluoromethyl group, a substituted or unsubstituted alkyl group, a substituted or unsubstituted alkylene group having a polymerizable functional group, and a polymerizable functional group, provided that at least one of R.sup.3 to R.sup.12 represents an electron-withdrawing group, and at least one of R.sup.1 to R.sup.12 has a polymerizable functional group.)

Method for resolution of citalopram intermediate 5-cyano diol

Provided is a method for resolution of formula 4-[4-dimethylamino-1-(4-fluorophenyl)-1-hydroxylbutyl]-3-hydroxy-methyl benzonitrile as an enantiomer thereof, comprising the following steps: a salt of (S)-4-[4-dimethylamino-1-(4-fluorophenyl)-1-hydroxylbutyl]-3-hydroxymethyl benzonitrile with a resolving agent D-(+)di-p-toluoyl tartaric acid was crystallized in a resolving solvent; the method is characterized in that the resolving solvent is an ether solvent. Also provided is a new crystal form of the resolved intermediate.

Method for resolution of citalopram intermediate 5-cyano diol

Provided is a method for resolution of formula 4-[4-dimethylamino-1-(4-fluorophenyl)-1-hydroxylbutyl]-3-hydroxy-methyl benzonitrile as an enantiomer thereof, comprising the following steps: a salt of (S)-4-[4-dimethylamino-1-(4-fluorophenyl)-1-hydroxylbutyl]-3-hydroxymethyl benzonitrile with a resolving agent D-(+)di-p-toluoyl tartaric acid was crystallized in a resolving solvent; the method is characterized in that the resolving solvent is an ether solvent. Also provided is a new crystal form of the resolved intermediate.

Method for resolution of citalopram intermediate 5-cyano diol

Provided is a method for resolution of formula 4-[4-dimethylamino-1-(4-fluorophenyl)-1-hydroxylbutyl]-3-hydroxy-methyl benzonitrile as an enantiomer thereof, comprising the following steps: a salt of (S)-4-[4-dimethylamino-1-(4-fluorophenyl)-1-hydroxylbutyl]-3-hydroxymethyl benzonitrile with a resolving agent D-(+)di-p-toluoyl tartaric acid was crystallized in a resolving solvent; the method is characterized in that the resolving solvent is an ether solvent. Also provided is a new crystal form of the resolved intermediate.

METHOD FOR PURIFYING KEY INTERMEDIATES OF CITALOPRAM

The present invention relates to a method for purifying key intermediates of Citalopram, i.e. 4-[4-(dimethylamino)-1-(4-fluorophenyl)-1-hydroxybutyl]-3-hydroxymethylbenzonitrile and a salt thereof. The method comprises dissolving crude 4-[4-(dimethylamino)-1-(4-fluorophenyl)-1-hydroxybutyl]-3-hydroxymethylbenzonitrile (compound of formula I containing formaldehyde impurity) with an organic solvent, adding a washing solution, controlling the temperature, stirring, leaving to stand for layering, and removing the aqueous layer, so as to obtain a purified organic solution of 4-[4-(dimethylamino)-1-(4-fluorophenyl)-1-hydroxybutyl]-3-hydroxymethylbenzonitrile. The method provided by the present invention can effectively remove aldehyde group-containing impurities in the intermediate. The method of the present invention has the advantages of simple operation, cheap raw materials and mild conditions, and is suitable for large-scale industrial production.

METHOD FOR PURIFYING KEY INTERMEDIATES OF CITALOPRAM

The present invention relates to a method for purifying key intermediates of Citalopram, i.e. 4-[4-(dimethylamino)-1-(4-fluorophenyl)-1-hydroxybutyl]-3-hydroxymethylbenzonitrile and a salt thereof. The method comprises dissolving crude 4-[4-(dimethylamino)-1-(4-fluorophenyl)-1-hydroxybutyl]-3-hydroxymethylbenzonitrile (compound of formula I containing formaldehyde impurity) with an organic solvent, adding a washing solution, controlling the temperature, stirring, leaving to stand for layering, and removing the aqueous layer, so as to obtain a purified organic solution of 4-[4-(dimethylamino)-1-(4-fluorophenyl)-1-hydroxybutyl]-3-hydroxymethylbenzonitrile. The method provided by the present invention can effectively remove aldehyde group-containing impurities in the intermediate. The method of the present invention has the advantages of simple operation, cheap raw materials and mild conditions, and is suitable for large-scale industrial production.