摘要:
The present invention provides a process for the production of a compound of formula: ##STR1## in which X and Y, independently, are hydrogen, halogen, NO.sub.2, CF.sub.3, CN, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, COO--C.sub.1 -C.sub.4 alkyl, CO--C.sub.1 -C.sub.4 alkyl, NH--(C.sub.1 -C.sub.4 alkyl), N(C.sub.1 -C.sub.4 alkyl).sub.2, NH(C.sub.1 -C.sub.4 alkyl-OH), N(C.sub.1 -C.sub.4 alkyl-OH).sub.2, COOH or SO.sub.3 H or an ester or amide thereof, or COOM or SO.sub.3 M in which M is Na, K, Ca, Mg, ammonium, mono-, di-, tri- or tetra-C.sub.1 -C.sub.4 alkylammonium, mono-, di- or tri-hydroxyalkylammonium or ammonium that is di- or tri-substituted with a mixture of C.sub.1 -C.sub.4 alkyl and C.sub.1 -C.sub.4 hydroxyalkyl groups;Z is hydrogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, CF.sub.3, halogen (F, Cl, Br, I), SO.sub.3 H or SO.sub.3 M in which M has its previous significance; andn is 1 or 2; comprisingA) reacting a diazonium compound having the formula: ##STR2## in which X and n have their previous significance and G is a counter ion, with ethylene in the presence of an inorganic or organic palladium compound, or a mixture thereof, as catalyst-precursor, to produce a compound having the formula: ##STR3## in which X and n have their previous significance; and B) reacting 2 moles of the compound of formula (3) with 1 mole of a compound having the formula: ##STR4## In which Z has its previous significance and each R.sub.1 is the same and is a bromine or iodine atom, in the presence of an inorganic or organic palladium compound, or a mixture thereof, as catalyst-precursor, to produce a compound having the formula (1). The compounds of formula (1) are useful as fluorescent whitening agents.
摘要:
A process for the production of a fluorescent whitening agent of formula: ##STR1## in which X and Z are as defined herein, comprising A) rearranging a hydrazobenzene compound having the formula: ##STR2## in which Z is as defined herein, to produce in situ a compound having the formula: ##STR3## B) diazotising the compound of formula (3) to produce a compound having the formula: ##STR4## in which Z has its previous significance and G.sub.1 is a counter ion; and C) reacting the compound of formula (4) with 2 moles of a compound having the formula: ##STR5## in which X and n have their previous significance, in the presence of an inorganic or organic palladium salt, or a mixture thereof, as catalyst-precursor, to produce a compound having the formula (1).
摘要:
Process for the coupling of a) nucleophiles selected from the group alcohols, thioles, amines, metallised hydrocarbons, CH-acidic compounds and metal cyanides, or of b) carbon monoxide mixed with water, alcohols, ammonia, primary or secondary amines, to organic compounds selected from the group of leaving-group-containing aromatics, hetero-aromatics with a C-bonded leaving group, aromatic or hetero-aromatic methyl compounds with a leaving group bonded to the methyl group, ethylenically unsaturated organic compounds with a C-bonded leaving group, or organic allyl compounds with a leaving group in allyl position, or c) vinyl compounds with leaving-group-containing aromatics, whilst cleaving the leaving group in the presence of Pd complexes with monophospholine ligands as the catalyst, whereby variants b) and c) are carried out in the presence of an inorganic base or organic nitrogen base, the process being characterised in that the Pd complex contains secondary monophosphines with aliphatic, branched or cyclic substituents as ligands.
摘要:
Process for the coupling of a) nucleophiles selected from the group alcohols, thioles, amines, metallised hydrocarbons, CH-acidic compounds and metal cyanides, or of b) carbon monoxide mixed with water, alcohols, ammonia, primary or secondary amines, to organic compounds selected from the group of leaving-group-containing aromatics, hetero-aromatics with a C-bonded leaving group, aromatic or hetero-aromatic methyl compounds with a leaving group bonded to the methyl group, ethylenically unsaturated organic compounds with a C-bonded leaving group, or organic allyl compounds with a leaving group in allyl position, or c) vinyl compounds with leaving-group-containing aromatics, whilst cleaving the leaving group in the presence of Pd complexes with monophospholine ligands as the catalyst, whereby variants b) and c) are carried out in the presence of an inorganic base or organic nitrogen base, the process being characterised in that the Pd complex contains secondary monophosphines with aliphatic, branched or cyclic substituents as ligands.
摘要:
A process for the preparation of primary aromatic carboxamides by the carbonylation of an aromatic compound, which contains at least one leaving group, with carbon monoxide, in the presence of a homogeneous or heterogeneous Pd catalyst and at least stoichiometric amounts of an amidation agent at elevated temperatures, which is characterized in that a primary carboxamide or a primary urethane is used as the amidation agent, and the reaction is carried out in the presence of an acylation catalyst.
摘要:
The present invention provides a non-covalent coupling method for the preparation of sterically stabilized lipsomes which may be used for targeted drug delivery, e.g., pegylated liposomes. The method simplifies the attachment of targeting vectors to sterically stabilized liposomes. The present invention also provides a liposome composition comprising a compound of the formula and a compound of the formula Z-Y, wherein Z is any compound capable of binding to a cellular receptor, and X and Y are compounds which can interact with each other non-convalently, and wherein the substituents n, F1 and F2 are as provided in the specification.
摘要:
The present invention provides a non-covalent coupling method for the preparation of sterically stabilized lipsomes which may be used for targeted drug delivery, e.g., pegylated liposomes. The method simplifies the attachment of targeting vectors to sterically stabilized liposomes. The present invention also provides a liposome composition comprising a compound of the formula and a compound of the formula Z-Y, wherein Z is any compound capable of binding to a cellular receptor, and X and Y are compounds which can interact with each other non-convalently, and wherein the substituents n, F1 and F2 are as provided in the specification.
摘要:
The present invention relates to a first compound having the formula wherein R is halogen, R1S(O)n or (R1)2NC(X)O; R1 is C1-C8alkyl, C1-C8haloalkyl, aryl-C1-C8-alkyl or aryl; n is 0, 1, 2 or 3; X is O or S; and R3 is C2-C5alkyl or C1-C5haloalkyl, or a salt thereof. The present invention is also directed to a second compound having the formula wherein R is fluorine, bromine, iodine, R1S(O)n or (R1)2NC(X)O; R1 is C1-C8alkyl, C1-C8- haloalkyl, aryl-C1-C8alkyl or aryl; n is 0, 1, 2 or 3; X is O or S; and R2 is hydrogen, C1-C4alkyl or C1-C4haloalkyl, with the proviso that R1 is different from C1-C8 alkyl or aryl if X is S, R is different from iodine if R2 is methyl, and R is different from fluorine, bromine or iodine if R2 is hydrogen.
摘要:
Process for the preparation of compounds of formula (I) wherein R is halogen, R1O1R1S(O)n or (R1)2NC(X)O; R1 is C1-C8alkly, aryl-C1-C8alkyl, C1-C8haloalkyl or aryl; n is 0, 1, 2 or 3; X is O or S; and R2 is hydrogen, C1-C4alkyl or C1-C4haloalkyl, in which process, in a solvent, (1) an aniline derivative of formula (IV) wherein R is as defined above, and R3 is C1-C5alkyl or C1-C5haloalkyl, is diazotised in the presence of a mineral acid to form the corresponding diazonium salt of formul (II) wherein R and R3 are as defined above, Am− is an anion, and m is 1 or 2, (2) the resulting diazonium salt of formula (II) is carbonylated in the presence of a catalyst, CO and optionally a buffer, to form a benzoic acid derivative of formula (III) wherein R and R3 are as defined above, and (3) the benzoic acid derivative of formula (III) is then subjected to benzylic lactonisation in the ortho-position alkyl chain R3 in the presence of a free-radical initiator and a halogenating agent.
摘要翻译:制备式(I)化合物的方法,其中R是卤素,R 1,R 1,R 1,S(O) n或(R 1)2 NC(X)O; R 1是C 1 -C 8烷基,芳基-C 1 -C 8烷基, C 1 -C 8烷基,C 1 -C 8卤代烷基或芳基; n为0,1,2或3; X是O或S; R 2是氢,C 1 -C 4烷基或C 1 -C 4烷基, 其中在溶剂中,(1)式(Ⅳ)的苯胺衍生物,其中R如上定义,R 3是C 1 H 3 C 1 -C 5烷基或C 1 -C 5卤代烷基在无机酸存在下重氮化,形成相应的重氮盐 式(II)其中R和R 3如上所定义,A m - 是阴离子,m是1或2,(2)所得到的重氮盐 在催化剂CO和任选的缓冲剂存在下将式(II)羰基化以形成式(III)的苯甲酸衍生物,其中R和R 3如上定义,和(3 )然后在自由基引发剂和卤化剂的存在下,在邻位烷基链R 3 3上对式(III)的苯甲酸衍生物进行苄基内酯化。
摘要:
The invention relates to novel N-phenyl-4-(4-pyridyl)-2-pyrimidineamine derivatives of the general formula (I) wherein the sum of (m+p) together is 0, 1, 2 or 3; n and q are independently of each other 0 or 1, and the sum of (m+p+q) together is 1, 2, 3 or 4; R1 is hydrogen, halogen, alkoxy, haloalkyl, haloalkoxy or alkyl; R2 is hydrogen, C1–C6-alkyl, C1–C6-haloalkyl or C1–C6-alkoxy; R2A is hydrogen, C1–C6-alkyl, C3–C4-alkenyl or C3–C4-alkynyl; each of R3, R4, R5 and R6 is, independently of the others, hydrogen, C1–C6-alkyl, C1–C6-haloalkyl, hydroxy-C1–C6-alkyl or C1–C6-alkoxy-C1–C6-alkyl, or the ring members CR3R4 or CR5R6 or CR2R2A are independently of each other a carbonyl group (C═O) or a group C═S; X is C═O, C═S, S═O or O═S═O; Y is O, S, C═O, CH2, —N(R8)—, —O—N(R8)—, —N(R8)—O— or NH—; R7 is hydrogen, C1–C4-alkyl, C3–C4-alkenyl, C3–C4-alkynyl, —CH2OR8, CH2SR8, —C(O)R8, —C(O)OR8, SO2R8, SOR8 or SR8; and R8 is C1–C8-alkyl, C1–C8-alkoxyalkyl, C1–C8 haloalkyl or phenylC1–C2-alkyl wherein the phenyl may be substituted by up to three groups selected from halo or C1–C4-alkyl; or a salt thereof. The invention also relates to the preparation of the compounds and to agrochemical compositions comprising at least one of those compounds as active ingredient as well as the preparation of the said compositions and to the use of the compounds or of the compositions in controlling or preventing the infestation of plants by phytopathogenic microorganisms, especially fungi.