Patent classifications
C07D239/30
Substituted 1,2,3-Triylidenetris(cyanomethanylylidene) Cyclopropanes for VTE, Electronic Devices and Semiconducting Materials Using Them
The present invention relates to a process for preparation of an electrically doped semiconducting material comprising a [3]-radialene p-dopant or for preparation of an electronic device containing a layer comprising a [3]-radialene p-dopant, the process comprising the steps: (i) loading an evaporation source with the [3]-radialene p-dopant; and (ii) evaporating the [3]-radialene p-dopant at an elevated temperature and at a reduced pressure, wherein the [3]-radialene p-dopant is selected from compounds having a structure according to formula (I) wherein A.sup.1 and A.sup.2 are independently aryl- or heteroaryl-substituted cyanomethylidene groups, the aryl and/or heteroaryl is selected independently in A.sup.1 and A.sup.2 from 4-cyano-2,3,5,6-tetrafluorphenyl,2,3,5,6-tetrafluorpyridine-4-yl, 4-trifluormethyl-2,3,5,6-tetrafluorphenyl, 2,4-bis(trifluormethyl)-3,5,6-trifluorphenyl, 2,5-bis(trifluormethyl)-3,4,6-trifluorphenyl, 2,4,6-tris(trifluormethyl)-1,3-diazine-5-yl, 3,4-dicyano-2,5,6-trifluorphenyl, 2-cyano-3,5,6-trifluorpyridine-4-yl, 2-trifluormethyl-3,5,6-trifluorpyridine-4-yl, 2,5,6-trifluor-1,3-diazine-4-yl and 3-trifluormethyl-4-cyano-2,5,6-trifluophenyl), and at least one aryl or heteroaryl is 2,3,5,6-tetrafluorpirydine-4-yl, 2,4-bis(trifluormethyl)-3,5,6-trifluorphenyl, 2,5-bis(trifluormethyl)-3,4,6-trifluorphenyl, 2,4,6-tris(trifluormethyl)-1,3-diazine-5-yl, 3,4-dicyano-2,5,6-trifluorphenyl, 2-cyano-3,5,6-trifluorpyridine-4-yl, 2-trifluormethyl-3,5,6-trifluorphenyl, provided that the heteroaryl in both A.sup.1 and A.sup.2 cannot be 2,3,5,6-tetrafluorpyridine-4-yl at the same time, respective [3]-radialene compounds, and semiconducting materials and layer, and electronic devices comprising said compounds.
##STR00001##
Substituted 1,2,3-Triylidenetris(cyanomethanylylidene) Cyclopropanes for VTE, Electronic Devices and Semiconducting Materials Using Them
The present invention relates to a process for preparation of an electrically doped semiconducting material comprising a [3]-radialene p-dopant or for preparation of an electronic device containing a layer comprising a [3]-radialene p-dopant, the process comprising the steps: (i) loading an evaporation source with the [3]-radialene p-dopant; and (ii) evaporating the [3]-radialene p-dopant at an elevated temperature and at a reduced pressure, wherein the [3]-radialene p-dopant is selected from compounds having a structure according to formula (I) wherein A.sup.1 and A.sup.2 are independently aryl- or heteroaryl-substituted cyanomethylidene groups, the aryl and/or heteroaryl is selected independently in A.sup.1 and A.sup.2 from 4-cyano-2,3,5,6-tetrafluorphenyl,2,3,5,6-tetrafluorpyridine-4-yl, 4-trifluormethyl-2,3,5,6-tetrafluorphenyl, 2,4-bis(trifluormethyl)-3,5,6-trifluorphenyl, 2,5-bis(trifluormethyl)-3,4,6-trifluorphenyl, 2,4,6-tris(trifluormethyl)-1,3-diazine-5-yl, 3,4-dicyano-2,5,6-trifluorphenyl, 2-cyano-3,5,6-trifluorpyridine-4-yl, 2-trifluormethyl-3,5,6-trifluorpyridine-4-yl, 2,5,6-trifluor-1,3-diazine-4-yl and 3-trifluormethyl-4-cyano-2,5,6-trifluophenyl), and at least one aryl or heteroaryl is 2,3,5,6-tetrafluorpirydine-4-yl, 2,4-bis(trifluormethyl)-3,5,6-trifluorphenyl, 2,5-bis(trifluormethyl)-3,4,6-trifluorphenyl, 2,4,6-tris(trifluormethyl)-1,3-diazine-5-yl, 3,4-dicyano-2,5,6-trifluorphenyl, 2-cyano-3,5,6-trifluorpyridine-4-yl, 2-trifluormethyl-3,5,6-trifluorphenyl, provided that the heteroaryl in both A.sup.1 and A.sup.2 cannot be 2,3,5,6-tetrafluorpyridine-4-yl at the same time, respective [3]-radialene compounds, and semiconducting materials and layer, and electronic devices comprising said compounds.
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Methods for Rapid Formation of Chemicals Including Positron Emission Tomography Biomarkers
Methods for rapid, efficient, and safe fluoridation and radiolabeling of established and new biomarkers are described. More specifically, the described herein methods may be used for fluoridation of biomarkers or to facilitate isotopic exchanges, especially .sup.19F/.sup.18F IEX, for rapid and efficient manufacturing of radiotracers, including radiotracers for positron emission tomography (PET), under clinically relevant conditions.
TRIAZINE AND PYRIMIDINE (THIO)AMIDES AS FUNGICIDAL COMPOUNDS
The present disclosure relates to triazine and pyrimidine (thio)amide compounds, processes and intermediates for their preparation as well as the uses thereof for controlling phytopathogenic microorganisms, such as phytopathogenic fungi.
HERBICIDAL COMPOUNDS
The present invention relates to a compound of formula (I) 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, R.sup.10, R.sup.11 and G are as defined herein; and wherein the compound of formula (I) is optionally present as an agrochemically acceptable salt thereof. These compounds are suitable for use as herbicides. The invention therefore also relates to a method of controlling weeds, especially grassy monocotyledonous weeds, in crops of useful plants, comprising applying a compound of formula (I), or a herbicidal composition comprising such a compound, to the plants or to the locus thereof.
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PHARMACEUTICAL PROCESS AND INTERMEDIATES
The present disclosure concerns the large-scale manufacture of pharmaceutical compounds, and novel intermediates for use in the manufacture. International Patent Application WO2011154737 discloses morpholine pyrimidines useful for treating cancer, processes for their preparation and pharmaceutical compositions thereof. In particular, WO2011154737 discloses, as experimental Example 2.02 on page 60, the compound 4-{4-[(3R)-3-methylmorpholin-4-yl]-6-[1-((R)—S-methylsulfonimidoyl)cyclopropyl]pyrimidin-2-yl}-1H-pyrrolo[2,3-b]pyridine (hereafter referred to as the compound of Formula (I)). The structure of the compound of Formula (I) is shown below. A synthetic route to the compound of Formula (I) is described at pages 51 to 57, 66 and 67 of WO2011154737, and is summarised below in Scheme 1.
##STR00001##
Amide compound and pharmaceutical comprising same
Provided is a novel compound which has an excellent Aβ aggregation inhibitory effect and is useful as a pharmaceutical. An amide compound represented by the formula (1) or a salt thereof, wherein Z represents CH or N; A and B are the same or different and each represents —CH.sub.2—, —O—, —S—, or —NH—; R.sup.1 and R.sup.2 are the same or different and each represents a branched alkyl group, a branched alkenyl group, an optionally substituted aromatic hydrocarbon group, an optionally substituted aralkyl group, an optionally substituted cycloalkyl group, or an optionally substituted aromatic heterocyclic group; and R.sup.3 represents a branched alkyl group, a branched alkenyl group, an optionally substituted cycloalkyl group, or an optionally substituted aralkyl group. ##STR00001##
Amide compound and pharmaceutical comprising same
Provided is a novel compound which has an excellent Aβ aggregation inhibitory effect and is useful as a pharmaceutical. An amide compound represented by the formula (1) or a salt thereof, wherein Z represents CH or N; A and B are the same or different and each represents —CH.sub.2—, —O—, —S—, or —NH—; R.sup.1 and R.sup.2 are the same or different and each represents a branched alkyl group, a branched alkenyl group, an optionally substituted aromatic hydrocarbon group, an optionally substituted aralkyl group, an optionally substituted cycloalkyl group, or an optionally substituted aromatic heterocyclic group; and R.sup.3 represents a branched alkyl group, a branched alkenyl group, an optionally substituted cycloalkyl group, or an optionally substituted aralkyl group. ##STR00001##
PTEFb inhibiting macrocyclic compounds
The present invention relates to novel modified macrocyclic compounds with improved tolerability of general formula (I) as described and defined herein, and methods for their preparation, their use for the treatment and/or prophylaxis of disorders, in particular of hyper-proliferative disorders and/or virally induced infectious diseases and/or of cardiovascular diseases. The invention further relates to intermediate compounds useful in the preparation of said compounds of general formula (I). ##STR00001##
PTEFb inhibiting macrocyclic compounds
The present invention relates to novel modified macrocyclic compounds with improved tolerability of general formula (I) as described and defined herein, and methods for their preparation, their use for the treatment and/or prophylaxis of disorders, in particular of hyper-proliferative disorders and/or virally induced infectious diseases and/or of cardiovascular diseases. The invention further relates to intermediate compounds useful in the preparation of said compounds of general formula (I). ##STR00001##