摘要:
A process for the preparation of a compound of formula (I) wherein: R is an alkynyl group; R1 is alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkyl-alkyl, phenyl and phenylalkyl, it being possible in turn for all of the receding groups to carry one or more identical or different halogen atoms; alkoxy; alkenyloxy; alkynyloxy; alkoxyalkyl; haloalkoxy; alkylthio; haloalkylthio; alkysulfonyl; formyl; alkanoyl; hydroxy; halogen; cyano; nitro; amino; alkylamino; dialkylamino; carboxyl; alkoxycarbonyl; alkenyloxycarbonyl; or alkynyloxycarbonyl; and n is an integer from 0 to 3, said process comprising: (i) the reaction of a compound of formula (III) wherein R, R1 and n are as hereinbefore defined; m and m′ are independently 0 or 1; when m and m′ are both 0, A is an alkyl, alkenyl or alkynyl group (suitably having up to eight carbon atoms), optionally substituted by one or more groups independently selected from halogen, hydroxy, alkoxy, C1-4 dialkylamino or cyano; when one of m and m′ is 0 and the other is 1, A is an alkanediyl, alkenediyl or alkynediyl group containing at least two carbon atoms (and suitably having up to eight carbon atoms), optionally substituted by one or more groups independently selected from halogen, hydroxy, alkoxy, C1-4 dialkylamino or cyano; when m and m′ are both 1, A is an alkanetriyl, alkenetriyl or alkynetriyl group containing at least three carbon atoms (and suitably having up to eight carbon atoms), optionally substituted by one or more groups independently selected from halogen, hydroxy, alkoxy, C1-4 dialkylamino or cyano; and wherein if the group A contains three or more carbon atoms, one or more of the carbon atoms may each optionally be replaced with an oxygen atom, provided that there is at least one carbon atom between any two oxygen atoms in the molecule, with a compound of formula (IV) to give a compound of formula (II) wherein R, R1 and n are as hereinbefore defined, and (ii) the reaction of a compound of formula (II) with, wherein L is a leaving group, to give the compound of formula (I) as hereinbefore defined, is disclosed.
摘要:
The invention relates to &agr;-sulfin- and &agr;-sulfonamino acid amides of the general formula I including the optical isomers thereof and mixtures of such isomers, wherein n is a number zero or one; R1 is C1-C12alkyl, C1-C12alkyl substituted with C1-C4alkoxy, C1-C4alkylthio, C1-C4alkylsulfonyl, C3-C8cycloalkyl, cyano, C1-C6alkoxycarbonyl, C3-C6alkenyloxycarbonyl or C3-C6alkenyloxycarbonyl; C3-C8cycloalkyl; C2-C12alkenyl; C2-C12alkynyl; C1-C12haloalkyl; or a group NR12R13 wherein R12 and R13 are each independently of the other hydrogen or C1-C6-alkyl, or together are tetra- or penta-methylene; R2 and R3 are each independently hydrogen; C1-C8alkyl; C1-C8alkyl substituted with hydroxy, mercapto, C1-C4alkoxy or C1-C4alkylthio; C3-C8alkenyl; C3-C8alkynyl; C3-C8cycloalkyl; C3-C8cycloalkyl-C1-C4alkyl; or the two groups R2 and R3 together with the carbon atom to which they are bonded form a three- to eight-membered hydrocarbon ring; R4, R5, R6 and R7 are each independently hydrogen or C1-C4alkyl; R8 is C1-C6alkyl, C3-C6alkenyl or C3-C6alkynyl; R9, R10, R14, R15, R16 and R17 are each independently hydrogen or C1-C4alkyl; A is optionally substituted phenyl, and to the preparation of those substances and to agrochemical compositions comprising at least one of those compounds as active ingredient. The invention relates also to 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.
摘要翻译:本发明涉及包含其光学异构体的通式I的α-亚磺酸和α-磺氨基酰胺和这些异构体的混合物,其中n是数个零或一个; R 1是C 1 -C 12烷基,被C 1 -C 12取代的C 1 -C 12烷基, C 4烷氧基,C 1 -C 4烷硫基,C 1 -C 4烷基磺酰基,C 3 -C 8环烷基,氰基,C 1 -C 6烷氧基羰基,C 3 -C 6烯氧基羰基或C 3 -C 6烯氧基羰基; C 3 -C 8环烷基; C 2 -C 12烯基; C 2 -C 12炔基; C 1 -C 12卤代烷基; 或NR 12 R 13基团,其中R 12和R 13各自独立地为氢或C 1 -C 6 - 烷基,或一起为四或五亚甲基; R 2和R 3各自独立地为氢; C1-C8烷基; 被羟基,巯基,C 1 -C 4烷氧基或C 1 -C 4烷硫基取代的C 1 -C 8烷基; C3-C8链烯基; C3-C8炔基; C 3 -C 8环烷基; C 3 -C 8环烷基-C 1 -C 4烷基; 或两个R 2和R 3与它们所键合的碳原子一起形成三至八元烃环; R 4,R 5,R 6和R 7各自独立地为氢或C 1 -C 4烷基; R 8为C 1 -C 6烷基, C 3 -C 6烯基或C 3 -C 6炔基; R 9,R 10,R 14,R 15,R 16和R 17各自独立地为氢或C 1 -C 4烷基; A为任选取代的苯基,并且为这些物质的制备以及包含至少一种 化合物作为活性成分。 本发明还涉及所述组合物的制备以及化合物或组合物在控制或预防植物病原微生物特别是真菌侵染植物中的用途。
摘要:
The invention relates to &agr;-sulfin- and &agr;-sulfonamino acid amides of the general formula I including the optical isomers thereof and mixtures of such isomers, wherein n is a number zero or one; R1 is C1-C12alkyl, C1-C12alkyl substituted with C1-C4alkoxy, C1-C4alkylthio, C1-C4alkylsulfonyl, C3-C8cycloalkyl, cyano, C1-C6alkoxycarbonyl, C3-C6alkenyloxycarbonyl or C3-C6alkynyloxycarbonyl; C3-C8cycloalkyl; C2-C12alkenyl; C2-C12alkynyl; C1-C12haloalkyl; or a group NR12R13 wherein R12 and R13 are each independently of the other hydrogen or C1-C6-alkyl, or together are tetra- or penta-methylene; R2 and R3 are each independently hydrogen; C1-C8alkyl; C1-C8alkyl substituted with hydroxy, mercapto, C1-C4alkoxy or C1-C4alkylthio; C3-C8alkenyl; C3-C8alkynyl; C3-C8cycloalkyl; C3-C8cycloalkyl-C1-C4alkyl; or the two groups R2 and R3 together with the carbon atom to which they are bonded form a three- to eight-membered hydrocarbon ring; R4, R5, R6 and R7 are each independently hydrogen or C1-C4alkyl; R8 is C1-C6alkyl, C3-C6alkenyl or C3-C6alkynyl; R9 and R10 are each independently hydrogen or C1-C4alkyl; and R11 is either in wherein R14, R,15, R16 and R17 are each independently hydrogen or C1-C4alkyl, X is oxygen, sulfur or —NR18—, wherein R18 is hydrogen or C1-C4alkyl, and A is optionally substituted mono- or polycylic aryl or heteroaryl, and to the preparation of those substances and to agrochemical compositions comprising at least one of those compounds as active ingredient. The invention relates also to the preparation of 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.
摘要翻译:本发明涉及包含其光学异构体的通式I的α-亚磺酸和α-磺氨基酰胺和这些异构体的混合物,其中n是数个零或一个; R 1是C 1 -C 12烷基,被C 1 -C 12取代的C 1 -C 12烷基, C4烷氧基,C1-C4烷硫基,C1-C4烷基磺酰基,C3-C8环烷基,氰基,C1-C6烷氧基羰基,C3-C6烯氧基羰基或C3-C6炔氧基羰基; C 3 -C 8环烷基; C 2 -C 12烯基; C 2 -C 12炔基; C 1 -C 12卤代烷基; 或NR 12 R 13基团,其中R 12和R 13各自独立地为氢或C 1 -C 6 - 烷基,或一起为四或五亚甲基; R 2和R 3各自独立地为氢; C1-C8烷基; 被羟基,巯基,C 1 -C 4烷氧基或C 1 -C 4烷硫基取代的C 1 -C 8烷基; C3-C8链烯基; C3-C8炔基; C 3 -C 8环烷基; C 3 -C 8环烷基-C 1 -C 4烷基; 或两个R 2和R 3与它们所键合的碳原子一起形成三至八元烃环; R 4,R 5,R 6和R 7各自独立地为氢或C 1 -C 4烷基; R 8为C 1 -C 6烷基, C 3 -C 6烯基或C 3 -C 6炔基; R 9和R 10各自独立地为氢或C 1 -C 4烷基; 并且R 11在其中R 14,R 15,R 16和R 17各自独立地为氢或C 1 -C 4烷基,X为氧,硫或-NR 18 - ,其中R 18为氢或C 1 -C 4烷基,A为任选取代的单或多环芳基 或杂芳基,以及这些物质的制备以及包含这些化合物中的至少一种作为活性成分的农药组合物。 本发明还涉及组合物的制备以及化合物或组合物在通过植物病原微生物特别是真菌控制或预防植物感染中的用途。
摘要:
The invention relates to novel pesticidally active compounds of the general formula I as well as possible isomers and mixtures of isomers thereof, wherein n is a number zero or one; and R1 is C1-C12alkyl that is unsubstituted or may be substituted by C1-C4alkoxy, C1-C4alkylthio, C1-C4alkylsulfonyl, C3-C8cycloalkyl, cyano, C1C6alkoxycarbonyl, C3-C6alkenyloxycarbonyl or by C3-C6alkynyloxycarbonyl; C3-C8cycloalkyl; C2-C12alkenyl; C2-C12alkynyl; C1-C12haloalkyl: or a group NR11R12 wherein R11 and R12 are each independently of the other hydrogen or C1-C8alkyl, or together are tetra- or penta-methylene; R2 and R3 are each independently of the other hydrogen; C1-C8alkyl; C1-C8alkyl substituted by hydroxy, C1-C4alkoxy, mercapto or by C1-C4alkylthio; C3-C8alkenyl; C3-C8alkynyl; C3-C8cycloalkyl; C3-C8cycloalkyl-C1-C4alkyl; or the two groups R2 and R3 together with the carbon atom to which they are bonded form a three- to eight-membered ring; R4, R5, R6 and R7 are identical or different and are each independently of the others hydrogen or C1-C4alkyl; R8 is C1-C6alkyl, C3-C6alkenyl or C3-C6alkynyl; A is C1-C6alkylene; and B is optionally mono- or poly-nuclear, unsubstituted or substituted aryl; optionally mono- or poly-nuclear, unsubstituted or substituted heteroaryl; C4-C12alkyl; or C3-C8cycloalkyl. The novel compounds have plant-protecting properties and are suitable for protecting plants against infestation by phytopathogenic microorganisms.
摘要:
Propargylether derivatives of formula I including the optical isomers thereof and mixtures of such isomers, wherein R1 is hydrogen, alkyl, cycloalkyl or optionally substituted aryl, R2 and R3 are each independently hydrogen or alkyl, R4 is alkyl, alkenyl or alkynyl, R5, R6, R7, and R8 are each independently hydrogen or alkyl and R9 is a group R10 is optionally substituted aryl or optionally substituted heteroaryl, R11 is hydrogen or optionally substituted alkyl, alkenyl or alkynyl, Z is hydrogen —CO—R16, —COOR16, —CO—COOR16 or —CONR16R17, R12 is hydrogen, or optionally substituted alkyl, alkenyl or alkynyl, R13 is hydrogen or alkyl, R14 is hydrogen, alkyl, cycloalkyl or cycloalkyl-alkyl, R15 is alkyl, alkenyl, alkynyl, optionally substituted aryl or optionally substituted aryl-alkyl, and R16 and R17 are independently of each other hydrogen, optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted aryl or optionally substituted heteroaryl, have been found to be useful for controlling or preventing the infestation of plants by phytopathogenic microorganisms, especially fungi. The invention relates the novel compounds and also to the preparation thereof and to the use of the compounds for plant protection, and to compositions suitable for applying the novel compounds in agricultural techniques.
摘要:
Compounds of the formula I in which: where: X is CH or N; Y is O; S, S═O or NR5; Z is OR2, SR2, N(R3)R4; or Y and Z together form 5- to 7-membered ring which contains, 2 or 3 hetero atoms O and/or N and which is unsubstituted or substituted by C1-C4alkyl, halo-C1-C4alkyl, halogen, ═O or cyclopropyl; V is a direct bond or C1-C6alkylene, which is unsubstituted or substituted by C1-C3alkyl, C2-C3alkylidene or C3-C6cycloalkylidene; U is O, S, NR7, SO or SO2; W is substituted or unsubstituted aryl or substituted or unsubstituted heteroaryl; R1 is cyclopropyl, C1C6alkyl or halo-C1-C6alkyl; R2 and R3 independently of one another are C1-C6alkyl or halo-C1-C6alkyl; R4 and R5 independently of one another are hydrogen, C1-C6alkyl or C1-C6alkoxy; R7 is hydrogen, C1-C6alkyl, benzyl, C1-C6alkylcarbonyl, halo-C1-C6alkylcarbonyl, halo-C2-C6alkenylcarbonyl; R21 and R22 independently of one another are hydrogen, halogen, C1-C8alkyl or C1-C8alkoxy or C1-C8alkylthio; R23, R24, R25, R26 independently of one another are hydrogen, halogen, C1-C8alkyl or C1-C8alkoxy; are pesticidally active. They can be used for pest control, in particular as fungicides, acaricides and insecticides in crop protection.
摘要翻译:式Iin的化合物,其中:其中:X为CH或N; Y为O; S,S = O或NR5; Z是OR2,SR2,N(R3)R4; 或Y和Z一起形成5-至7-元环,其含有2或3个杂原子O和/或N,并且其未被取代或被C 1 -C 4烷基,卤代-C 1 -C 4烷基,卤素,O或环丙基取代; V C 1 -C 3亚烷基或C 3 -C 6亚烷基; U是O,S,NR 7,SO或SO 2; W是取代或未取代的芳基或取代或未取代的杂芳基 R 1和R 2各自独立地为C 1 -C 6烷基或卤代-C 1 -C 6烷基; R 4和R 5彼此独立地为氢,C 1 -C 6烷基或C 1 -C 6烷氧基; R 7为 R 2和R 22彼此独立地是氢,卤素,C 1 -C 8烷基或C 1 -C 8烷氧基或C 1 -C 8烷硫基; R 23是氢,C 1 -C 6烷基,苄基,C 1 -C 6烷基羰基,卤代C 1 -C 6烷基羰基 R 24,R 25,R 26彼此独立地是氢,卤素,C 1 -C 8烷基或C 1 -C 8烷氧基; 具有杀虫活性,可用于防治害虫,特别是杀虫剂,杀螨剂和作物保护中的杀虫剂。
摘要:
.alpha.-Amino acid amides of the formula I ##STR1## in which n is the number zero or one;R.sub.1 is C.sub.1 -C.sub.12 alkyl, which is unsubstituted or can be substituted by C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 alkylthio, C.sub.1 -C.sub.4 alkylsulfonyl, C.sub.3 -C.sub.8 cycloalkyl, cyano, C.sub.1 -C.sub.6 alkoxycarbonyl, C.sub.3 -C.sub.6 alkenyloxycarbonyl or C.sub.3 -C.sub.6 alkynyloxycarbonyl; C.sub.3 -C.sub.8 cycloalkyl; C.sub.2 -C.sub.12 alkenyl; C.sub.2 -C.sub.12 alkynyl; C.sub.1 -C.sub.12 halogenoalkyl or a group NR.sub.13 R.sub.14 ; in whichR.sub.13 and R.sub.14 independently of one another are hydrogen or C.sub.1 -C.sub.6 alkyl or together are tetra- or pentamethylene;R.sub.2 and R.sub.3 independently of one another are hydrogen; C.sub.1 -C.sub.8 alkyl; C.sub.1 -C.sub.8 alkyl which is substituted by hydroxyl, C.sub.1 -C.sub.4 alkoxy, mercapto or C.sub.1 -C.sub.4 alkylthio; C.sub.3 -C.sub.8 alkenyl; C.sub.3 -C.sub.8 alkynyl; C.sub.3 -C.sub.8 cycloalkyl or C.sub.3 -C.sub.8 cycloalkyl-C.sub.1 -C.sub.4 alkyl, or in which the two groups R.sub.2 and R.sub.3, together with the carbon atom to which they are bonded, form a three- to eight-membered carbocyclic ring;R.sub.4 is hydrogen or C.sub.1 -C.sub.6 alkyl;R.sub.5 is hydrogen; C.sub.1 -C.sub.6 alkyl or phenyl, which is unsubstituted or can be substituted by halogen, nitro, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 halogenoalkyl, C.sub.1 -C.sub.4 alkoxy or C.sub.1 -C.sub.4 alkylthio; andR.sub.6 is a group G ##STR2## in which R.sub.7 and R.sub.8 independently of one another are hydrogen or C.sub.1 -C.sub.6 alkyl;p is the number zero or one; andR.sub.9, R.sub.10 and R.sub.11 independently of one another are hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 halogenoalkyl, C.sub.3 -C.sub.6 alkenyl, C.sub.3 -C.sub.6 alkynyl, C.sub.1 -C.sub.6 alkoxy, C.sub.3 -C.sub.6 alkenyloxy, C.sub.3 -C.sub.6 alkynyloxy, C.sub.1 -C.sub.6 alkylthio, halogen or nitro are valuable microbicides. They can be employed in crop protection in the form of suitable compositions, for example for controlling fungal diseases.
摘要:
The present invention relates to a process for the preparation of compounds of formula I wherein R1 and R2 are each independently of the other hydrogen or C1-C5alkyl and R3 is CF3 or CF2H, by a) reaction of a compound of formula II wherein R1 and R2 are as defined for formula I, with at least one reducing agent to form a compound of formula wherein R1 and R2 are as defined for formula I, and b) reaction of that compound with at least one reducing agent to form a compound of formula IV wherein R1 and R2 are as defined for formula I, and (c) reaction of that compound with a compound of formula V wherein Q is chlorine, fluorine, bromine, iodine, hydroxy or C1-C6alkoxy and R3 is as defined for formula I, to form the compound of formula I; and to novel intermediates for use in that process.
摘要:
The present invention relates to a process for the preparation of syn-enriched 5-amino-9-isopropyl-benzonorbomene in which the ratio of compounds of formula (Ia(syn)) to compounds of formula (Ib(anti)) is from 70:30 to 99:1, which process comprises reacting a compound of formula (Il) in a pressure vessel with hydrogen in the presence of a palladium catalyst and a solvent, at a pressure of at least 2 bar and a temperature of from 00 C to 45° C., to form syn-enriched 5-amino-9-isopropyl-benzonorbomene.
摘要:
The invention concerns a novel process for the preparation of 2-phenyl-2-hydroxy-N-[2-(3-alkoxy-4-hydroxyphenyl)-ethyl]-acetamides of the formula (I), wherein R1 is alkyl, R2 and R3 are each independently hydrogen or alkyl, and R4 is optionally substituted aryl or optionally substituted heteroaryl, which process comprises reacting a 2-(3-alkoxy-4-hydroxyphenyl)-ethylamine of the formula (II), wherein R1 R2 and R3 are as defined above with a α-hydoxycarboxylic acid ester of the formula (III) or a dioxolanone of the formula (III)a, wherein R4 is as defined above, and R5, R6 and R7 independently of each other are lower alkyl. The compounds of formula (I) are important intermediates for a novel group of fungicides derived from mandelic acid amides.