Heterocyclic imidazolyl vinyl ethers and use of same as fungicides or
bactericides
    1.
    发明授权
    Heterocyclic imidazolyl vinyl ethers and use of same as fungicides or bactericides 失效
    杂环咪唑基乙烯基醚,用作杀真菌剂或杀菌剂

    公开(公告)号:US4330545A

    公开(公告)日:1982-05-18

    申请号:US150964

    申请日:1980-05-19

    CPC分类号: C07C43/225 A01N43/50

    摘要: Aryl-imidazol-1-yl vinyl ethers and their acid addition salts are disclosed, wherein the imidazolyl vinyl ether has the formula: ##STR1## Ar in the formula represents a substituted or unsubstituted aryl or heterocyclic radical; R represents hydrogen or a C.sub.1 -C.sub.12 alkyl or cycloalkyl (saturated or unsaturated) or Ar as above; Im represents a 1-H-imidazol-1-yl group (unsubstituted or substituted); and Y represents a saturated or unsaturated C.sub.1 -C.sub.12 alkyl or a group --Z--Ar in which Ar has the above meaning and --Z-- is a saturated or unsaturated C.sub.1 -C.sub.12 alkylene wherein each of the alkyl and the alkylene may have a carbon chain once or twice interrupted by or, in the case of the alkylene, terminated on its Ar-end by oxy, thio, sulfinyl or sulfonyl bridges, always with the proviso that at least one of Ar and Y is a heterocyclic radical. These compounds are wide-spectrum fungicides and bactericides, and the preferred compounds among them are hydrophilic.

    摘要翻译: 公开了芳基 - 咪唑-1-基乙烯基醚及其酸加成盐,其中咪唑基乙烯基醚具有下式:下式中的Ar表示取代或未取代的芳基或杂环基; R代表氢或C1-C12烷基或环烷基(饱和或不饱和)或如上所述的Ar; Im表示1-H-咪唑-1-基(未取代或取代的); 并且Y表示饱和或不饱和的C 1 -C 12烷基或基团-Z-Ar,其中Ar具有上述含义,-Z-是饱和或不饱和的C 1 -C 12亚烷基,其中烷基和亚烷基中的每一个可以具有碳 链中断一次或两次,或者在亚烷基的情况下,通过氧基,硫基,亚磺酰基或磺酰基桥接在其Ar末端上,条件是Ar和Y中的至少一个是杂环基。 这些化合物是广谱杀菌剂和杀菌剂,其中优选的化合物是亲水的。

    Aryl imidazolyl vinyl ethers and processes for using same
    2.
    发明授权
    Aryl imidazolyl vinyl ethers and processes for using same 失效
    芳基咪唑基乙烯基醚及其使用方法

    公开(公告)号:US4210657A

    公开(公告)日:1980-07-01

    申请号:US970330

    申请日:1978-12-18

    摘要: Aryl-imidazol-1-yl vinyl ethers and their acid addition salts are disclosed, wherein the imidazolyl vinyl ether has the formula: ##STR1## Ar in the formula represents a substituted or unsubstituted aryl or heterocyclic radical; R represents hydrogen or a C.sub.1 -C.sub.12 alkyl or cycloalkyl (saturated or unsaturated) or Ar as above; Im represents a 1-H-imidazol-1-yl group (unsubstituted or substituted); and Y represents a saturated or unsaturated, acyclic or cyclic C.sub.1 -C.sub.12 alkyl, or aryl or aralkyl, or an alkyl or alkylene residue directly bound to the ether oxygen and having a chain once or twice interrupted by --O--, --S--, --SO-- or --SO.sub.2 -- bridges. These compounds are effective wide spectrum fungicides and bactericides.

    摘要翻译: 公开了芳基 - 咪唑-1-基乙烯基醚及其酸加成盐,其中咪唑基乙烯基醚具有下式:式中的Ar表示取代或未取代的芳基或杂环基; R代表氢或C1-C12烷基或环烷基(饱和或不饱和)或如上所述的Ar; Im表示1-H-咪唑-1-基(未取代或取代的); 并且Y表示饱和或不饱和的无环或环状C 1 -C 12烷基或芳基或芳烷基,或直接键合到醚氧上并具有一个或两个被-O - , - S - 间隔的链的烷基或亚烷基, -SO-或-SO 2 - 桥。 这些化合物是有效的广谱杀菌剂和杀菌剂。

    Thioethers
    3.
    发明授权
    Thioethers 失效
    硫醚

    公开(公告)号:US4131608A

    公开(公告)日:1978-12-26

    申请号:US795224

    申请日:1977-05-09

    摘要: This invention relates to novel thioethers as well as to the addition salts thereof with inorganic or organic acids. The novel compounds and their addition salts have valuable anti-mycotic and fungicidal properties. Further the invention relates to a process for preparing the novel compounds and their addition salts, and to anti-mycotic and fungicidal compositions containing the novel thioethers, or addition salts thereof, as the active constituent.

    摘要翻译: 本发明涉及新型硫醚以及其与无机或有机酸的加成盐。 新化合物及其加成盐具有有价值的抗真菌和杀真菌性能。 此外,本发明涉及一种制备新化合物及其加成盐的方法,以及含有新型硫醚或其加成盐作为活性成分的抗霉菌和杀真菌组合物。

    Imidazolyl vinyl ethers and process for preparing same
    5.
    发明授权
    Imidazolyl vinyl ethers and process for preparing same 失效
    咪唑基乙烯基醚及其制备方法

    公开(公告)号:US4210656A

    公开(公告)日:1980-07-01

    申请号:US970312

    申请日:1978-12-18

    摘要: .alpha.-Aryl-.beta.-imidazol-1-yl vinyl ethers and their acid addition salts are disclosed, wherein the imidazolyl vinyl ether has the formula: ##STR1## Ar represents a substituted or unsubstituted aryl group, R an alkyl, aryl or aralkyl group, X an oxygen atom, a sulfur atom, a sulfinyl or a sulfonyl group and R1 a lower alkyl group or a nitro group. These compounds are effective wide spectrum fungicides and bactericides. To prepare these vinyl ethers, a corresponding 1-arylacylimidazole is o-alkylated in presence of NaH with a corresponding .alpha.-halogen ether, .alpha.-halogen thioether, .alpha.-halogen sulfinyl compound or a corresponding .alpha.-halogen sulfonyl compound.

    摘要翻译: 公开了α-氨基-β-咪唑-1-基乙烯基醚及其酸加成盐,其中咪唑基乙烯基醚具有下式:Ar表示取代或未取代的芳基,R是烷基,芳基或芳烷基 X为氧原子,硫原子,亚磺酰基或磺酰基,R 1为低级烷基或硝基。 这些化合物是有效的广谱杀菌剂和杀菌剂。 为了制备这些乙烯基醚,相应的1-芳基酰基咪唑在NaH存在下与相应的α-卤代醚,α-卤代硫醚,α-卤代亚磺酰基化合物或相应的α-卤代磺酰化合物进行邻烷基化。

    Method for production of imidazolyl vinyl ethers
    6.
    发明授权
    Method for production of imidazolyl vinyl ethers 失效
    咪唑基乙烯基醚的制备方法

    公开(公告)号:US4554356A

    公开(公告)日:1985-11-19

    申请号:US692324

    申请日:1985-01-16

    CPC分类号: C07D231/12 C07D249/08

    摘要: A process for the manufacture of imidazolylvinyl ethers of the formula ##STR1## wherein Im represents the substituted or unsubstituted 1-H-imidazol-1-yl group and An, R and Y are defined hereinbelow by condensation of a corresponding ketone of the formulaAr--CO--CHR--Im (II)with the splitting-off of a Z group, with a condensable substance of the formulaZ--Y (III)in the aqueous solution of a strong inorganic base, preferably in concentrated aqueous soda lye. The reaction may also be carried out in the presence of a second liquid organic phase, preferably benzene or toluene, especially in the presence of a phase transfer catalyst in this case. Through careful crystallization of the product manufactured according to this method, it is possible to manufacture approximately pure E-isomers of the imidazolylvinyl ether of formula (I), without the requirement of chromatographic separation.

    摘要翻译: PCT No.PCT / EP82 / 00010 Sec。 371日期1982年5月24日 102(e)日期1982年5月24日PCT提交1982年1月21日PCT公布。 出版物WO82 / 02552 日本1982年8月5日。一种制备式(I)的咪唑基乙烯基醚的方法,其中Im表示取代或未取代的1-H-咪唑-1-基,An,R和Y定义如下 通过将式Ar-CO-CHR-Im(II)的相应的酮与Z基团的分离与式ZY(III)的可冷凝物质在强无机碱的水溶液中缩合, 优选在浓缩的苏打碱液中。 反应也可以在第二液体有机相存在下进行,优选苯或甲苯,特别是在这种情况下在相转移催化剂存在下。 通过根据该方法制造的产品的仔细结晶,可以制备式(I)的咪唑基乙烯基醚的近似纯的E-异构体,而不需要色谱分离。

    Theophylline derivatives
    7.
    发明授权
    Theophylline derivatives 失效
    茶碱衍生物

    公开(公告)号:US4603204A

    公开(公告)日:1986-07-29

    申请号:US474230

    申请日:1983-03-11

    CPC分类号: C07D473/08

    摘要: New derivatives of theophylline having the formula ##STR1## in which R denotes hydrogen or OH, n the numbers 0 or 1, X either >CH-- or >N--, Y either --O-- or --CO-- and R a five membered or six membered aryl ring or hetero-aryl ring, that is substituted in given cases with halogen, short chain alkyl groups, alkoxy groups or halogen-alkyl, and exhibit in addition to other properties, histamine-, serotinine- bradykynine- antagonistic, anti-anaphylactic and -adrenergic stimulating effects.

    摘要翻译: 具有式(I)的茶碱的新衍生物,其中R表示氢或OH,n为数字0或1,X或> CH-或> N-,Y为-O-或-CO-,R a 在给定的情况下被卤素,短链烷基,烷氧基或卤素 - 烷基取代的五元或六元芳基环或杂芳基环,并且除了其它性质外,还表现出组胺,血清素 - 卡那霉素拮抗剂 ,抗过敏和肾上腺素能刺激作用。

    Imidazole ethyl oxyalkoxy derivatives and thio analogues thereof
    9.
    发明授权
    Imidazole ethyl oxyalkoxy derivatives and thio analogues thereof 失效
    咪唑乙氧基烷氧基衍生物及其硫代类似物

    公开(公告)号:US4177350A

    公开(公告)日:1979-12-04

    申请号:US950825

    申请日:1978-10-12

    摘要: Antimycotically and antibacterially effective imidazole derivatives of the formula (1) ##STR1## in which R.sup.1, R.sup.2 and R.sup.3 are the same or different and are hydrogen and lower alkyl; R.sup.4 is hydrogen, lower alkyl or selected from unsubstituted or substituted cycloalkyl, benzyl and phenyl groups wherein the substituents are selected from halogen, lower alkyl, lower alkoxy, lower alkylthio, phenyl, cyano, nitro and amino, or wherein R.sup.4 is an unsubstituted or halosubstituted pyridyl, R.sup.5 is nitro or lower alkyl in any unsubstituted position of the imidazole ring, Ar is a phenyl group optionally substituted with at least one substituent which is halogen, lower alkyl, lower alkoxy or a C.sub.4 -C.sub.8 cycloalkyl, or wherein Ar is a benzyl group optionally substituted with a substituent of the type set forth for R.sup.4, X and Y are independently selected from oxygen (--O--) or sulfur (--S), n is an integer of from 1 to 5 inclusive and p is Zero or an integer of from 1 to 3 inclusive, and the addition salts of formula (1) compounds with pharmaceutically acceptable organic or inorganic acids; the formula (1) compounds and their addition salts as specified have a relatively low oral toxicity or/and an improved solubility and are suitable for use in human and veterinary medicine and for chemo-agricultural fungus control purposes. Suitable pharmaceutical compositions including the novel derivatives or/and their addition salts with acceptable acids as well as methods for producing such novel derivatives are disclosed.

    摘要翻译: 式(1)的抗真菌和抗菌有效的咪唑衍生物其中R 1,R 2和R 3相同或不同,为氢和低级烷基; R4是氢,低级烷基或选自未取代或取代的环烷基,苄基和苯基,其中取代基选自卤素,低级烷基,低级烷氧基,低级烷硫基,苯基,氰基,硝基和氨基,或其中R4是未取代或未取代的 卤素取代的吡啶基,R5是咪唑环的任何未取代的位置的硝基或低级烷基,Ar是任选被至少一个取代基取代的苯基,该取代基是卤素,低级烷基,低级烷氧基或C 4 -C 8环烷基,或其中Ar是 任选被R4,X和Y所示类型的取代基取代的苄基独立地选自氧(-O-)或硫(-S),n为1至5的整数,p为零 或1〜3的整数,式(1)化合物与药学上可接受的有机酸或无机酸的加成盐; 式(1)化合物及其加成盐具有相对较低的口服毒性或/和改善的溶解性,适用于人兽药和化学农药真菌控制目的。 公开了包括新型衍生物和/或其与可接受的酸的加成盐的合适的药物组合物以及用于制备这些新型衍生物的方法。

    Imidazolyl-oxime ethers having anti-mycotic and bactericidal activity
    10.
    发明授权
    Imidazolyl-oxime ethers having anti-mycotic and bactericidal activity 失效
    具有抗真菌和杀菌活性的咪唑基 - 肟醚

    公开(公告)号:US4124767A

    公开(公告)日:1978-11-07

    申请号:US754691

    申请日:1976-12-27

    摘要: Imidazolyl oxime ethers (I) are disclosed which contain an aromatic or heteroaromatic grouping linked to the carbon atom of the oxime ether, the oxime being etherified by a variety of groups; aliphatic, aromatic, heteroaromatic, cycloaliphatic and aliphatic substituted by aromatic, heteroaromatic or cycloaliphatic groups. The compounds are obtained from the corresponding ketones by reaction with O-substituted hydroxylamines or by reaction of metal oximates with halides of the required etherifying group. The said products (I) possess antimycotic and bactericidal activity.

    摘要翻译: 公开了咪唑基肟醚(I),其含有与肟醚的碳原子连接的芳族或杂芳族基团,肟由各种基团醚化; 脂族,芳族,杂芳族,脂环族和被芳族,杂芳族或脂环族基团取代的脂族。 通过与O-取代的羟胺反应或通过金属肟酸酯与所需醚化基团的卤化物的反应,从相应的酮获得化合物。 所述产物(I)具有抗真菌和杀菌活性。