摘要:
5-[(4-chlorophenyl)methyl]-2,2-dimethylcyclopentanone is produced by reacting 1-[(4-chlorophenyl)methyl]-3-methyl-2-oxocyclopentanecarboxylic acid methyl ester or 1-[(4-chlorophenyl)methyl]-3-methyl-2-oxocyclopentanecarboxylic acid ethyl ester with sodium hydride and methyl halide, then hydrolyzing the obtained 1-[(4-chlorophenyl)methyl]-3,3-dimethyl-2-oxocyclopentanecarboxylic acid methyl ester or 1-[(4-chlorophenyl)methyl]-3,3-dimethyl-2-oxocyclopentanecarboxylic acid ethyl ester. The process provides 5-[(4-chlorophenyl)methyl]-2,2-dimethylcyclopentanone, an important intermediate of an agricultural or horticultural fungicide, e.g., Metconazole.
摘要:
A process for preparing a derivative of azolylmethylcycloalkanol of the following formula (I) comprising, providing a solid-liquid two-phase mixture of a cycloalkanone derivative of formula (II), an azole compound of formula (III), a metal oxide of formula (IV), and an organic solvent, and adding a sulfonium compound of formula (V) to said solid-liquid two-phase mixture under heating while stirring, ##STR1## wherein R.sup.1 and R.sup.2 individually represent a hydrogen atom or an alkyl group; X is a halogen atom, an alkyl group, a haloalkyl group, a phenyl group, a cyano group, or a nitro group; m is an integer of 0 to 5 (when m is 2 or larger, Xs may be either the same or different); n is an integer of 0 to 2; A represents a nitrogen atom or a group CH; M.sup.1 represents an alkali metal atom or an alkaline earth metal atom; M.sup.2 represents an alkaline earth metal atom, a zinc atom, or two alkali metal atoms; Y represents a halogen atom or a C.sub.1 -C.sub.4 alkoxysulfonyloxy group; and p denotes an integer of 0 or 1.
摘要翻译:一种制备下式(I)的唑基甲基环烷醇衍生物的方法,包括:提供式(II)的环烷酮衍生物,式(III)的唑类化合物,式(III)的唑类化合物,式 (IV)和有机溶剂,并在搅拌下在加热下向所述固液两相混合物中加入式(Ⅴ)的锍化合物,(II)+(III)+ M 2 O (I)其中R 1和R 2各自表示氢原子或烷基; X是卤素原子,烷基,卤代烷基,苯基,氰基或硝基; m为0〜5的整数(当m为2以上时,X可以相同或不同); n为0〜2的整数, A表示氮原子或基团CH; M1表示碱金属原子或碱土金属原子; M2表示碱土金属原子,锌原子或两个碱金属原子; Y表示卤素原子或C1-C4烷氧基磺酰氧基; p表示0或1的整数。
摘要:
Disclosed is a 3-(unsubstituted or substituted benzyl)-1-alkyl-2-oxocyclopentane carboxylic acid alkyl ester derivative as represented by the general formula (I): ##STR1## where R.sup.1 and R.sup.2 are each a lower alkyl group;X is a halogen atom, a cyano group, an alkyl group, a haloalkyl group, a phenyl group or a nitro group; andm is 0 or an integer from 1 to 5 and when m is greater than 1 each X can be the same or different.Further, disclosed is a method for the preparation of the compound (I) by carrying out the benzylation, rearrangement, and alkylation from the 2-oxocyclopentane carboxylic acid alkyl ester derivative without isolation of any intermediate compound. In addition, a fungicide is provided in which the 3-(unsubstituted or substituted benzyl)-1-alkyl-2-oxocyclopentane carboxylic acid alkyl ester derivatives (I) is contained as an active ingredient.Furthermore, it can provide 2-(unsubstituted or substituted benzyl)-5-alkylcyclopentanone derivatives from the 3-(unsubstituted or substituted benzyl)-1-alkyl-2-oxocyclopentane carboxylic acid alkyl ester derivatives (I).
摘要:
Disclosed herein are azole derivatives or the salts thereof which are represented by the general formula (I): ##STR1## wherein X represents a halogen atom, an alkyl group having 1 to 5 carbon atoms, a haloalkyl group, a phenyl group, a cyano group, or a nitro group, Xs being either the same or different from each other; n represents an integer of 1 to 5; A represents a nitrogen atom or CH; and one of R.sub.1 and R.sub.2 represents an alkyl group having 1 to 5 carbon atoms and the other a hydrogen atom or an alkyl group having 1 to 5 carbon atoms, with the proviso that when n is 1 or 2, X does not represent a halogen atom, an alkyl group having 1 to 5 carbon atoms or a phenyl group, and mycocides comprising an effective amount of azole derivative or medically or veterinarily acceptable salt thereof, said azole derivative being represented by the general formula (II): ##STR2## wherein X represents a halogen atom, an alkyl group having 1 to 5 carbon atoms, a haloalkyl group, a phenyl group, a cyano group, or a nitro group, Xs being either the same or different from each other; n represents an integer of 0 to 5; A represents a nitrogen atom or CH; and R.sub.1 and R.sub.2 respectively represent a hydrogen atom or an alkyl group having 1 to 5 carbon atoms, and a diluent or a carrier which is medically or veterinarily acceptable.
摘要:
Derivatives of alkyl 3-(substituted or unsubstituted benzylidene)-1-alkyl-2-oxocylopentanecarboxylate of the following formula (I), ##STR1## wherein R.sup.1 and R.sup.2 individually represent a lower alkyl group; X is a halogen atom, a cyano group, an alkyl group, a haloalkyl group, a phenyl group, or a nitro group; and m is an integer of 0 to 5; provided when m is 2 or larger, Xs may be either the same or different. The compounds are useful themselves as an effective ingredient of antifungal compositions, and can be used for intermediates of agriculture chemicals and medicines.
摘要:
This invention provides a process for producing an optically active 1,2-diol derivative by optical resolution. The optically active 1,2-diol derivative of the formula (I) which is capable of utilizing as an intermediate of fungicidal optically-active azole derivatives can be produced by esterifying a 1,2-diol derivative of the formula (I) as a substrate with a carboxylic acid derivative of the formula (II) as a reagent in the presence of a lipase as a catalyst. ##STR1## wherein R.sup.1 is C1-C5 alkyl group, C3-C7 cycloalkyl group or C1-C5 haloalkyl group, R.sup.2 is C1-C3 alkyl group substituted by a phenyl group which may have one or two halogen atoms and/or C1-C4 alkyl groups, C2-C3 alkenyl group substituted by a phenyl group which may have one or two halogen atoms and/or C1-C4 alkyl groups, or C1-C3 alkyl group substituted by a phenoxy group which may have one or two halogen atoms and/or C1-C4 alkyl groups, R.sup.3 is C1-C10 alkyl group or aryl group, and R.sup.4 is hydrogen atom, C1-C5 alkyl group, C2-C4 alkenyl group or COR.sub.3.
摘要:
Novel N-benzoly-N'-halogenoloweralkylidenehydrazine derivatives of the general formula ##STR1## (in which X represents Cl or Br, and Y represents H, F, Cl, Br, CH.sub.3 or CHCl--CH.sub.3, provided that when X is Cl, Y is the above-defined member other than Cl).
摘要:
In the present invention, an optically active cis type 1,2-diol derivative of the following formula (I) is produced by reacting a cis type 1,2-diol derivative of the formula (I) with a carboxylic acid derivative of the formula (II) in the presence of a lipase: ##STR1## wherein R.sup.1 and R.sup.2 independently represent hydrogen atom or an alkyl group, X represents a halogen atom, a nitro group, a cyano group, an alkyl group, a haloalkyl group, or a phenyl group, and n represents an integer of from 0 to 5; R.sup.3 represents a C.sub.1 -C.sub.10 alkyl group or an aryl group, and R.sup.4 represents a hydrogen atom, a C.sub.1 -C.sub.5 alkyl group, a C.sub.2 -C.sub.4 alkenyl group, or COR.sub.3.The cis type means that the bond between the cyclopentane ring and the hydroxy group and the bond between the cyclopentane ring and the benzyl group reside in the same direction as that portrayed on the paper.The optically active cis type 1,2-diol derivative is used as an intermediate for producing an optically active cis type azole derivative of the formula (VII).
摘要:
Disclosed herein is a process for preparing a cis-azole derivative represented by the general formula (I) ##STR1## wherein R.sup.1 and R.sup.2 denote each a hydrogen atom or an alkyl group, R denotes a halogen atom, a nitro group, a cyano group, an alkyl group, a haloalkyl group or a phenyl group, A denotes a nitrogen atom or a methine group, and n stands for an integer of 1-5,which comprises reducing an azolylmethyloxabicyclohexane derivative represented by the general formula (VI) ##STR2## wherein R.sup.1, R.sup.2, R, A and n have the same meanings as defined above. A fungicidal composition comprising the azolylmethyloxabicyclohexane derivative represented by the above-mentioned general formula (VI) is also desclosed.
摘要:
Disclosed is a 1,3,2-dioxathiolan-S-oxide derivative as represented by the general formula (I): ##STR1## (where R.sub.1 and R.sub.2 are identical to or different from each other and each is a hydrogen atom or a lower alkyl group;X is a halogen atom, a cyano group, a lower alkyl group, a haloalkyl group or a phenyl group;m is 0 or an integer from 1 to 5; and when small m is greater than 1 each x can be the same or different andn is 1 or 2).A 1,3,2-dioxathiolan-2-oxide derivative of the compound as represented by the general formula (I-I) is prepared by reacting a hydroxymethylcyclopentanol derivative with thionyl chloride; and a 1,3,2-dioxathiolan-2,2-dioxide derivative (I-II) thereof is prepared by oxidizing the compound (I-I). The compounds (I) can be employed as fungicides and intermediate compounds for the preparation of azolylmethylcyclopentanol derivatives.