Patent classifications
C07C275/16
PROCESS FOR PREPARING DIISOCYANATES BASED ON LYSINE
The invention relates to a process for preparing a diisocyanate of the formula (A)
##STR00001## where R is selected from the group consisting of alkyl, aryl, and combinations thereof, comprising the following process steps in the indicated order; 1) providing an intermediate of the formula (B) with a process using lysine and urea
##STR00002##
and where R and each R′ are independently selected from the group consisting of alkyl, aryl, and combinations thereof; and 2) thermolytic cleavage of the intermediate of the formula (B), thereby affording the diisocyanate of the formula (A),
and also to the diisocyanate directly prepared therewith.
IMPROVED METHOD OF SYNTHESIS AND PURIFICATION OF CITRULLINE
This invention provides for synthesis of citrulline from a transition metal complex of ornithine using cyanate to derivatize the terminal amino group of ornithine. The invention also provides improved methods for purification of citrulline produced by reaction of cyanate with ornithine via the steps of reprecipitation of copper complex of citrulline, removal of the complexing metal by sulfide precipitation, activated carbon adsorption and antisolvent crystallization.
IMPROVED METHOD OF SYNTHESIS AND PURIFICATION OF CITRULLINE
This invention provides for synthesis of citrulline from a transition metal complex of ornithine using cyanate to derivatize the terminal amino group of ornithine. The invention also provides improved methods for purification of citrulline produced by reaction of cyanate with ornithine via the steps of reprecipitation of copper complex of citrulline, removal of the complexing metal by sulfide precipitation, activated carbon adsorption and antisolvent crystallization.
INHIBITORS OF INTEGRIN ALPHA 2 BETA 1 AND METHODS OF USE
Disclosed herein, inter alia, are inhibitors of integrin alpha 2 beta 1 and methods of using the same.
MARKING PRECURSOR WITH SQUARIC ACID COUPLING
The invention relates to a marking precursor incorporating a chelator or fluorination group for radiolabelling with 44Sc, 47Sc, 55Co, 62Cu, 64Cu, 67Cu, 66Ga, 67Ga, 68Ga, 89Zr, 86Y, 90Y, 90Nb, 99mTc, 111ln, 135Sm, 140Pr, 159Gd, 149Tb, 160Tb, 161Tb, 165Er, 166Dy, 166Ho, 175Yb, 177Lu, 186Re, 188Re, 213Bi and 225Ac or with 18F, 131I or 211At, and one or two biological targeting vectors which are coupled to the chelator or fluorinating group via one or more squaric acid groups.
18F-LABELED TRIAZOLE CONTAINING PSMA INHIBITORS
The present technology is directed to compounds, intermediates thereof, compositions thereof, medicaments thereof, and methods related to the imaging of mammalian tissue overexpressing PSMA. The compounds are of Formula I
##STR00001##
or a pharmaceutically acceptable salt thereof, wherein one of R.sup.1, R.sup.2, and R.sup.3 is
##STR00002##
and of Formula IV
##STR00003##
or a pharmaceutically acceptable salt thereof.
18F-LABELED TRIAZOLE CONTAINING PSMA INHIBITORS
The present technology is directed to compounds, intermediates thereof, compositions thereof, medicaments thereof, and methods related to the imaging of mammalian tissue overexpressing PSMA. The compounds are of Formula I
##STR00001##
or a pharmaceutically acceptable salt thereof, wherein one of R.sup.1, R.sup.2, and R.sup.3 is
##STR00002##
and of Formula IV
##STR00003##
or a pharmaceutically acceptable salt thereof.
Eicosanoid derivatives
The present invention provides compounds (n-3 PUFA derivatives) of formula (I): ##STR00001##
that modulate conditions associated with cardiac damage, especially cardiac arrhythmias.
Eicosanoid derivatives
The present invention provides compounds (n-3 PUFA derivatives) of formula (I): ##STR00001##
that modulate conditions associated with cardiac damage, especially cardiac arrhythmias.
Method for producing carbamate and method for producing isocyanate
The present invention provides a method for producing a carbamate that includes a step (1) and a step (2) described below: (1) a step of producing a compound (A) having a urea linkage, using an organic primary amine having at least one primary amino group per molecule and at least one compound selected from among carbon dioxide and carbonic acid derivatives, at a temperature lower than the thermal dissociation temperature of the urea linkage; and (2) a step of reacting the compound (A) with a carbonate ester to produce a carbamate.