Patent classifications
C07C205/57
Methods for the preparation of 6-aminoisoquinoline
Described are methods for the preparation of 6-aminoisoquinoline, a useful intermediate compound in the synthesis of kinase inhibitors.
One step process for regioselective synthesis of α-acyloxy carbonyls
A regioselective N-Heterocyclic Carbene (NHC) catalyzed one step process for high yield synthesis of α-acyloxy carbonyl compounds is disclosed. ##STR00001##
One step process for regioselective synthesis of α-acyloxy carbonyls
A regioselective N-Heterocyclic Carbene (NHC) catalyzed one step process for high yield synthesis of α-acyloxy carbonyl compounds is disclosed. ##STR00001##
COMPOSITIONS AND METHODS FOR IMAGING
The present disclosure provides compositions for in vivo imaging of hydrogen peroxide; and methods for detecting hydrogen peroxide in vivo. The compositions and methods find use in various diagnostic applications, which are also provided.
COMPOSITIONS AND METHODS FOR IMAGING
The present disclosure provides compositions for in vivo imaging of hydrogen peroxide; and methods for detecting hydrogen peroxide in vivo. The compositions and methods find use in various diagnostic applications, which are also provided.
METHODS OF SYNTHESIZING A PROSTACYCLIN ANALOG
The present invention provides processes for preparing a prostacyclin analogue of Formula (I) or a pharmaceutically acceptable salt thereof, wherein R.sup.10 is a linear or branched C.sub.1-6 alkyl. The processes of the present invention comprise steps that generate improved yields and fewer byproducts than traditional methods. The processes of the present invention employ reagents (e.g., the oxidizing reagent) that are less toxic that those used in the traditional methods (e.g., oxalyl chloride). Many of the processes of the present invention generate intermediates with improved e.e. and chemical purity; thereby eliminating the need of additional chromatography steps. And, the processes of the present invention are scalable to generate commercial quantities of the final compound.
METHODS OF SYNTHESIZING A PROSTACYCLIN ANALOG
The present invention provides processes for preparing a prostacyclin analogue of Formula (I) or a pharmaceutically acceptable salt thereof, wherein R.sup.10 is a linear or branched C.sub.1-6 alkyl. The processes of the present invention comprise steps that generate improved yields and fewer byproducts than traditional methods. The processes of the present invention employ reagents (e.g., the oxidizing reagent) that are less toxic that those used in the traditional methods (e.g., oxalyl chloride). Many of the processes of the present invention generate intermediates with improved e.e. and chemical purity; thereby eliminating the need of additional chromatography steps. And, the processes of the present invention are scalable to generate commercial quantities of the final compound.
Nitrodiarylethenes as fluorescence quenchers for nucleic acid probes
Fluorescence quenching nitrodiarylethene analogs are useful in oligonucleotide conjugates and probes. These analogs, whose absorption spectra are substantially blue-shifted relatively to emission spectra of common fluorophores (such as fluorescein), do not need to rely on spectral overlap of quencher absorbance and fluorophore's emission for their quenching abilities. The oligonucleotide-quencher conjugates may be used in detection methods for nucleic acid targets.
Nitrodiarylethenes as fluorescence quenchers for nucleic acid probes
Fluorescence quenching nitrodiarylethene analogs are useful in oligonucleotide conjugates and probes. These analogs, whose absorption spectra are substantially blue-shifted relatively to emission spectra of common fluorophores (such as fluorescein), do not need to rely on spectral overlap of quencher absorbance and fluorophore's emission for their quenching abilities. The oligonucleotide-quencher conjugates may be used in detection methods for nucleic acid targets.
PROCESS FOR THE SYNTHESIS OF NON-RACEMIC CYCLOHEXENES
This invention relates to a process for the synthesis of a non-racemic cyclohexene compound of formula (I) by a Diels-Alder reaction of a compound of formula (II) with a compound of formula (III) wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8, R.sup.9 and Y have the meanings as defined in the description in the presence of a catalyst comprising at least one m-valent metal cation M.sup.m+ wherein the metal M is selected from Scandium (Sc), Yttrium (Y), Lanthanum (La), Cerium (Ce), Praseodymium (Pr), Neodymium (Nd), Promethium (Pm), Samarium (Sm), Europium (Eu), Gadolinium 15 (Gd), Terbium (Tb), Dysprosium (Dy), Holmium (Ho), Erbium (Er), Thulium (Tm), Ytterbium (Yb), Lutetium (Lu), Gallium (Ga) and Indium (In), and m is an integer of 1, 2 or 3, and a chiral ligand of the formula (IV) wherein R.sup.10a, R.sup.10b, R.sup.10c, R.sup.10d, R.sup.10a′, R.sup.10b′, R.sup.10c′, R.sup.10d′, Z and Z′ have the meanings as defined in the description.