摘要:
Process for preparing nitriles by reacting N-alkylcarboxamides (RCO—NHR1) or ammonium salts of carboxylic acids (RCOO—NH3R1+) or carboxylic acids in the presence of alkylamines or ammonium salts (RCOOH+NH2R1, RCOOH+NH13R1+) respectively, R being an arbitrarily substituted linear or branched C1-C12-alkyl radical, a C3-C12 cycloalkyl radical or an alkenyl, alkynyl or aryl or heteroaryl radical and R1 being an arbitrary substituted, linear or branched C2-C1 alkyl radical, a C3-C12 cycloalkyl radical or an alkenyl or alkynyl radical, with phosphonic anhydrides in the presence of an optional base in an organic solvent at a temperature in the range from −30 to 180° C. In advantageous embodiments, the phosphonic anhydride is a 2,4,6-substituted 1,3,5,2,4,6-trioxatriphosphinane 2,4,6-trioxide of the formula (I)
摘要翻译:通过使N-烷基甲酰胺(RCO-NHR 1)或羧酸铵盐(RCOO-NH 3 R 1 +)反应制备腈的方法, )或羧酸在烷基胺或铵盐的存在下(RCOOH + NH 2 R 1,RCOOH + NH 3 R 1) + SUP>),R是任意取代的直链或支链C 1 -C 12 - 烷基,C 3 - C 12环烷基或链烯基,炔基或芳基或杂芳基,R 1是任意取代的直链或支链C 2 -C 烷基,C 3 -C 12 - 环烷基或链烯基或炔基与膦酸酐在任选的碱存在下反应 在有机溶剂中,在-30至180℃的温度范围内。在有利的实施方案中,膦酸酐是2,4,6-取代的1,3,5,2,4,6-三氧杂三磷杂环己烷2,4 式(I)的6-三氧化物,
摘要:
Process for preparing nitriles by reacting N-alkylcarboxamides (RCO—NHR1) or ammonium salts of carboxylic acids (RCOO—NH3R1+) or carboxylic acids in the presence of alkylamines or ammonium salts (RCOOH+NH2R1, RCOOH+NH3R1+), respectively, R being an arbitrarily substituted linear or branched C1-C12-alkyl radical, a C3-C12 cycloalkyl radical or an alkenyl, alkynyl or aryl or heteroaryl radical and R1 being an arbitrary substituted, linear or branched C2-C1 alkyl radical, a C3-C12 cycloalkyl radical or an alkenyl or alkynyl radical, with phosphonic anhydrides in the presence of an optional base in an organic solvent at a temperature in the range from −30 to 180° C. In advantageous embodiments, the phosphonic anhydride is a 2,4,6-substituted 1,3,5,2,4,6-trioxatriphosphinane 2,4,6-trioxide of the formula (I)
摘要:
Methods for producing furfural-4-boronic acid by the reaction of furfural acetals (I), which are substituted by halogen in position 4, with boronic acid esters or anhydrides, by the subsequent metalation of compound (I) and the simultaneous or subsequent reaction with a boronic acid ester or anhydride to form an acetal-protected furfural-4-boronic acid ester. This product is subjected to acid hydrolysis to form furfural-4-boronic acid. In the formulae: X represents chlorine, bromine or iodine; R represents a branched, unbranched and/or cyclic, optionally substituted C1-C20 alkyl group, an optionally substituted C6-C12 aryl group or an optionally substituted C3-C8 cycloalkyl group, the two groups R together can form a ring; R′, R″, R′″ independently of one another represent acylic or cyclic, branched or unbranched, optionally substituted C1-C20 alkyl groups, or optionally substituted aryl groups, optionally two of the groups R′, R″ and R′″ together form a ring, or represent additional groups B(OR)3.
摘要:
The invention relates to a method for producing alkyl-substituted aromatic and heteroaromatic compounds by cross-coupling alkyl boronic acids with aryl- or heteroaryl-halogenides or with aryl- or heteroaryl-sulfonates in the presence of a catalyst and of a Brönsted base in a solvent or solvent mixture.
摘要:
The invention relates to a method for producing aryl or heteroaryl amines, ethers or thioethers (III) by cross-coupling primary or secondary amities, alcohols or thioalcohols with substituted aryl or heteroaryl compounds (I) in the presence of a Brønsted base and a catalyst or a pre-catalyst containing a) a transition metal, a complex, a salt, or a compound of a transition metal from the group V, Mn, Fe, Co, Ni, Rh, Pd, Ir, Pt, and b) at least one sulfonated phosphane ligand in a solvent or a solvent mixture corresponding to Scheme 1 wherein Hal represents fluorine, chlorine, bromine, iodine, alkoxy, trifluoromethane sulfonate, nonafluorotrimethyl-methane sulfonate, methane sulfonate, 4-nitrobenzene sulfonate, benzene sulfonate, 2-naphthalene sulfonate, 3-nitrobenzene sulfonate, 4-nitrobenzene sulfonate, 4-chlorobenzene sulfonate, 2,4,6-triisopropylbenzene sulfonate or any other sulfonate, and X represents O, S or NR″. The invention also relates to novel phosphane ligands.
摘要:
The invention concerns a method for producing: a) nitriles of formula (II) and b) isonitriles of formula (III) by reacting: a) carboxylic acid amides (RCO—NH2), ammonium salts of carboxylic acids (RCOO—NH4+) or carboxylic acids in the presence of ammonia or ammonium salts (RCOOH+NH3, RCOOH+NH4+) or b) formamides (H—CO—NHR) or mixtures of amines with formic acid, with cyclic phosphonic acid anhydrides while eliminating water at a temperature ranging from −30 to +120° C., in which R represents an arbitrarily substituted linear or branched C1-C8 alkyl radical, a C3-C10 cycloalkyl radical, alkenyl radical, alkynyl radical or an aryl radical or heteroaryl radical. As a cyclic phosphonic acid anhydride, a 2,4,6,-substituted 1,3,5,2,4,6 -trioxatriphosphinane-2,4,6-trioxide of formula (I) is advantageously used, in which: x=3, 4 or 5; R′, independent of one another, represents open-chain or branched, saturated or unsaturated, straight-chain C1to C16 alkyl radicals or cyclic C3 to C16 alkyl radicals or aryl or heteroaryl.
摘要:
A process for the manufacture of aminocarbonyl boronic acids of formula (IV) by converting the compounds of formula (III) with a Brønsted base Y(OH)n in a solvent or a solvent mixture, in which Z represents an optionally substituted arylene, heteroarylene, alkene, heteroalkene, alkylidene, heteroalkylidene, alkenylidene, heteroalkenylidene, alkynylidene, arylalkylene, heteroarylalkylene, arylheteroalkylene, heteroarylheteroalkylene, alkylheteroarylene, heteroalkylheteroarylene, or alkylarylene group; Y represents a metal or ammonium cation of valence n with 0
摘要:
Process for preparing compounds by cross-coupling of enolizable carbonyl compounds, nitriles or their analogues with substituted aryl or heteroaryl compounds in the presence of a Brönsted base and of a catalyst or precatalyst containing a.) a transition metal, a complex, a salt or a compound of this transition metal from the group V, Mn, Fe, Co, Ni, Rh, Pd, Ir, Pt) and b.) at least one sulphonated phosphane ligand in a solvent or solvent mixture.
摘要:
The present invention relates to compounds of the Formula or a pharmaceutically acceptable salt, solvate, hydrate or formulation thereof. These compounds can be used for the inhibition of Factor Xa and for the treatment and/or prevention of diseases that are mediated by Factor Xa activity.