The invention relates to novel crystalline phases of 5,6-dichloro-2-(isopropylamino)-1-(β-L-ribofuranosyl)-1H-benzimidazole (Maribavir), pharmaceutical compositions thereof and their use in medical therapy.

The invention relates to novel crystalline phases of 5,6-dichloro-2-(isopropylamino)-1-(β-L-ribofuranosyl)-1H-benzimidazole (Maribavir), pharmaceutical compositions thereof and their use in medical therapy.

A compound having the following structure:

##STR00001##

wherein: R.sup.1 is a linker having the formula —(CH.sub.2).sub.n-L.sup.1-, wherein L.sup.1 contains 1-6 carbon atoms and at least one —NH— linkage and at least one oxygen-containing or sulfur-containing linkage, and n is an integer of 0-3; R.sup.2 is a group having the formula —C(Y)-E, wherein Y is O or S, and E is a hydrocarbon group and either: (i) at least one carbon-carbon or carbon-nitrogen unsaturated bond or (ii) at least one alkyl halide group; R.sup.3 is selected from H, NR′.sub.2, NHC(O)R′, and —(CH.sub.2).sub.p-T, wherein T contains at least one —NH— linkage; R.sup.a, R.sup.b, R.sup.c, R.sup.d, R.sup.e, and R.sup.f are independently selected from of H, hydrocarbon groups containing 1-3 carbon atoms, fluorine atom, and chlorine atom; X is N or CR.sup.9, wherein R.sup.9 is selected from H, hydrocarbon groups containing 1-3 carbon atoms, fluorine atom, and chlorine atom; and pharmaceutically acceptable salts thereof.

A compound having the following structure:

##STR00001##

wherein: R.sup.1 is a linker having the formula —(CH.sub.2).sub.n-L.sup.1-, wherein L.sup.1 contains 1-6 carbon atoms and at least one —NH— linkage and at least one oxygen-containing or sulfur-containing linkage, and n is an integer of 0-3; R.sup.2 is a group having the formula —C(Y)-E, wherein Y is O or S, and E is a hydrocarbon group and either: (i) at least one carbon-carbon or carbon-nitrogen unsaturated bond or (ii) at least one alkyl halide group; R.sup.3 is selected from H, NR′.sub.2, NHC(O)R′, and —(CH.sub.2).sub.p-T, wherein T contains at least one —NH— linkage; R.sup.a, R.sup.b, R.sup.c, R.sup.d, R.sup.e, and R.sup.f are independently selected from of H, hydrocarbon groups containing 1-3 carbon atoms, fluorine atom, and chlorine atom; X is N or CR.sup.9, wherein R.sup.9 is selected from H, hydrocarbon groups containing 1-3 carbon atoms, fluorine atom, and chlorine atom; and pharmaceutically acceptable salts thereof.

The present invention relates to the technical field of acetonitrile refining, and in particular, to an improved acetonitrile purification process for an ultrahigh performance liquid chromatography-mass spectrometer. The present invention provides an acetonitrile purification process. A high-purity finished product may be obtained by performing operations of oxidation, rectification adsorption, drying, reflux rectification and filtration on industrial acetonitrile and controlling related parameters such as temperature, flow and the like, continuous production is ensured, a light transmittance of the finished product in ultraviolet rays of 200 to 260 nm is greater than or equal to 95%, water and impurities in the industrial acetonitrile are removed, and the requirements of the ultrahigh performance liquid chromatography-mass spectrometer are met; moreover, by controlling process parameters and equipment.

The present invention relates to the technical field of acetonitrile refining, and in particular, to an improved acetonitrile purification process for an ultrahigh performance liquid chromatography-mass spectrometer. The present invention provides an acetonitrile purification process. A high-purity finished product may be obtained by performing operations of oxidation, rectification adsorption, drying, reflux rectification and filtration on industrial acetonitrile and controlling related parameters such as temperature, flow and the like, continuous production is ensured, a light transmittance of the finished product in ultraviolet rays of 200 to 260 nm is greater than or equal to 95%, water and impurities in the industrial acetonitrile are removed, and the requirements of the ultrahigh performance liquid chromatography-mass spectrometer are met; moreover, by controlling process parameters and equipment.

A process for producing acetonitrile, the process comprising dehydrating a feedstock stream comprising acetonitrile, acrylonitrile, allyl alcohol, and water (and optionally methanol) in a dehydration (first) column to yield a dehydrated acetonitrile stream comprising acetonitrile and acrylonitrile, less than 1 wt % allyl alcohol, and less than 50 wt % water, and optionally hydrogen cyanide; distilling the dehydrated acetonitrile stream in a lights (second) column to yield a distillate stream comprising lights, and a bottoms stream comprising acetonitrile, acrylonitrile, water, and optionally hydrogen cyanide and acrylonitrile; extracting the distillation bottoms stream in an extraction (third) column to yield a raffinate stream comprising acetonitrile and less than 200 ppm acrylonitrile and an extract stream comprising water and acrylonitrile; purifying the raffinate stream to yield a product acetonitrile stream.

A process for producing acetonitrile, the process comprising dehydrating a feedstock stream comprising acetonitrile, acrylonitrile, allyl alcohol, and water (and optionally methanol) in a dehydration (first) column to yield a dehydrated acetonitrile stream comprising acetonitrile and acrylonitrile, less than 1 wt % allyl alcohol, and less than 50 wt % water, and optionally hydrogen cyanide; distilling the dehydrated acetonitrile stream in a lights (second) column to yield a distillate stream comprising lights, and a bottoms stream comprising acetonitrile, acrylonitrile, water, and optionally hydrogen cyanide and acrylonitrile; extracting the distillation bottoms stream in an extraction (third) column to yield a raffinate stream comprising acetonitrile and less than 200 ppm acrylonitrile and an extract stream comprising water and acrylonitrile; purifying the raffinate stream to yield a product acetonitrile stream.

The present invention provides novel Ruthenium-based transition metal complex catalysts comprising specific ligands, their preparation and their use in hydrogenation processes. Such complex catalysts are inexpensive, thermally robust, and olefin selective.

The present invention provides novel Ruthenium-based transition metal complex catalysts comprising specific ligands, their preparation and their use in hydrogenation processes. Such complex catalysts are inexpensive, thermally robust, and olefin selective.