Production of monohydroxy monocyclic acetals and their esters
    51.
    发明授权
    Production of monohydroxy monocyclic acetals and their esters 失效
    制备单羟基单环缩醛及其酯

    公开(公告)号:US4876368A

    公开(公告)日:1989-10-24

    申请号:US197936

    申请日:1988-05-24

    摘要: A process is provided for the production of a monohydroxy monocyclic acetal, e.g., trimethylolpropane cyclic formal, of a trihydroxy alcohol, e.g., trimethylolpropane, and an aldehyde, e.g., formaldehyde, by subjecting a "heavier condensation product" of the trihydroxy alcohol and the aldehyde than the desired cyclic acetal, i.e., one having a higher molecular weight and boiling point, to acetal formation conditions. In a preferred embodiment, the product of reaction of the trihydroxy alcohol and aldehyde is treated to remove the desired monohydroxy monocyclic acetal product and at least part of the remainder comprising the heavier condensation product is recycled to the reaction together with a flesh supply of trihydroxy alcohol and aldehyde. The monohydroxy monocyclic acetal product may be further reacted to obtain a desired ester, e.g. trimethylolpropane cyclic formal acrylate, such as by transesterifying the acetal with a low boiling ester of the esterifying acid, e.g., methyl acrylate, using tetra-isopropyl orthotitanate as transesterification catalyst.

    Microbicidal triazolyl phenylethanone ketals
    53.
    发明授权
    Microbicidal triazolyl phenylethanone ketals 失效
    杀菌三唑基苯乙酮缩酮

    公开(公告)号:US4853399A

    公开(公告)日:1989-08-01

    申请号:US931289

    申请日:1986-11-17

    申请人: Adolf Hubele

    发明人: Adolf Hubele

    摘要: Novel substituted 2-(1H-1,2,4-triazolyl)-1-phenylethan-1-one ketals of the general formula ##STR1## wherein one of the two phenyl substituents is in 2-position and the other is in 4-position, and whereinR.sub.a is halogen, methyl or C.sub.1 -C.sub.3 haloalkoxy, andU and V are each independently of the other C.sub.1 -C.sub.12 alkyl, unsubstituted or substituted by halogen or C.sub.1 -C.sub.6 alkoxy, or together are an alkylene bridge selected from ##STR2## wherein R.sub.1 to R.sub.5 are as defined herein, and the acid addition salts and metal complex salts, have microbicidal properties and are especially suitable for controlling phytopathogenic microorganisms. They can be used in the form of plant protective or seed dressing agents for preventing or controlling plant pathogens.

    摘要翻译: 新颖的取代的2-(1H-1,2,4-三唑基)-1-苯乙基-1-酮缩酮,其通式为“IMAGE”,其中两个苯基取代基之一位于2-位,另一个在4-位, 位置,并且其中R a是卤素,甲基或C 1 -C 3卤代烷氧基,并且U和V各自独立地是未被取代的或被卤素或C 1 -C 6烷氧基取代的另一个C 1 -C 12烷基,或者一起是选自的亚烷基桥,其中 R1至R5如本文所定义,并且酸加成盐和金属络合盐具有杀微生物的性质,并且特别适合于控制植物病原微生物。 它们可以以植物保护剂或拌种剂的形式用于预防或控制植物病原体。

    Cyclic derivatives of alkyl dihydroxyalkylxanthenes
    56.
    发明授权
    Cyclic derivatives of alkyl dihydroxyalkylxanthenes 失效
    烷基二羟基烷基呫吨的环状衍生物

    公开(公告)号:US4713455A

    公开(公告)日:1987-12-15

    申请号:US848139

    申请日:1986-04-04

    摘要: Compounds of the formula ##STR1## wherein one of the radicals R.sup.1, R.sup.2 or R.sup.3 denotes a straight-chain alkyl group having 4 to 8 C atoms and two vicinal hydroxyl groups in the .omega.,.omega.-1 or .omega.-1,.omega.-2 positions and the two other radicals represent straight-chain or branched alkyl groups having up to 12 C atoms in the position of R.sup.1 and R.sup.3 and up to 4 C atoms in the position of R.sup.2, the total of C atoms in these two alkyl substituents being a maximum of 14, are prepared by oxidation of the corresponding alkenylxanthines and by alkylation with compounds which introduce the dihydroxyalkyl radical or a precursor thereof. The dihydroxyalkyldialkylxanthines are suitable for the treatment of obstructive respiratory tract diseases.

    摘要翻译: 式(I)的化合物其中基团R 1,R 2或R 3中的一个表示具有4至8个C原子的直链烷基和ω,ω-1或ω-1中的两个邻位羟基, ω-2位,另外两个基团表示在R 2和R 3的位置具有至多12个C原子的直链或支链烷基,R2的位置中具有至多4个C原子的直链或支链烷基,这两个基团中的C原子总数 通过氧化相应的链烯基黄嘌呤并通过引入二羟基烷基或其前体的化合物进行烷基化来制备最多14个的烷基取代基。 二羟基烷基二烷基黄嘌呤适用于治疗阻塞性呼吸道疾病。

    Phenoxine-ketal ethers, compositions containing them and the use thereof
    57.
    发明授权
    Phenoxine-ketal ethers, compositions containing them and the use thereof 失效
    苯氧基 - 缩酮醚,含有它们的组合物及其用途

    公开(公告)号:US4707182A

    公开(公告)日:1987-11-17

    申请号:US733353

    申请日:1985-05-13

    摘要: The oxime ethers of the formula I below are able to act as antidotes or safeners to protect cultivated plants from the phytotoxic effects of herbicides. Such cultivated plants are preferably sorghum, cereals, maize and rice, and herbicides are principally chloroacetanilides and thiocarbamates. The oxime ethers have the formula I ##STR1## wherein n is 1 or 2, each of R.sub.1 and R.sub.2 is hydrogen or C.sub.1 -C.sub.4 alkyl each of R.sub.3 and R.sub.4 is hydrogen, halogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 haloalkyl, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 haloalkoxy, C.sub.1 -C.sub.4 alkylthio, C.sub.1 -C.sub.4 haloalkylthio, C.sub.1 -C.sub.4 alkylsulfinyl, C.sub.1 -C.sub.4 alkylsulfonyl, C.sub.1 -C.sub.4 haloalkylsulfinyl, C.sub.1 -C.sub.4 haloalkylsulfonyl or nitro; each of R.sub.5 and R.sub.6 independently of the other is C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 haloalkyl, C.sub.2 -C.sub.8 alkoxyalkyl, C.sub.3 -C.sub.4 alkenyl, C.sub.3 -C.sub.4 alkynyl, or together form a 2- to 6-membered alkylene or alkenylene bridge which may be substituted by 1 to 4 C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 haloalkyl, C.sub.1 -C.sub.4 alkoxy, C.sub.2 -C.sub.4 alkenyloxy, C.sub.2 -C.sub.8 alkoxyalkyl or C.sub.3 -C.sub.8 alkenyloxyalkyl groups; each of A and B independently of the other is oxygen or sulfur, or one of A and B is the methine group, X is a fluorinated C.sub.1 -C.sub.3 alkyl radical which may also additionally contain chlorine, and Y is hydrogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 haloalkyl, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 haloalkoxy or phenyl.

    摘要翻译: 以下式I的肟醚能够用作解毒剂或安全剂,以保护栽培植物免受除草剂的植物毒性作用。 这样的栽培植物优选是高粱,谷物,玉米和水稻,除草剂主要是氯乙酰苯胺和硫代氨基甲酸盐。 肟醚具有式I(I)其中n为1或2,R 1和R 2各自为氢或R 3和R 4各自为C 1 -C 4烷基,卤素,C 1 -C 4烷基,C 1 -C 4 卤代烷基,C1-C4烷氧基,C1-C4卤代烷氧基,C1-C4烷硫基,C1-C4卤代烷硫基,C1-C4烷基亚磺酰基,C1-C4烷基磺酰基,C1-C4卤代烷基亚磺酰基,C1-C4卤代烷基磺酰基或硝基; R 5和R 6各自独立地是C 1 -C 4烷基,C 1 -C 4卤代烷基,C 2 -C 8烷氧基烷基,C 3 -C 4烯基,C 3 -C 4炔基,或一起形成2-至6-元亚烷基或亚烯基桥,其中 可以被1至4个C 1 -C 4烷基,C 1 -C 4卤代烷基,C 1 -C 4烷氧基,C 2 -C 4烯氧基,C 2 -C 8烷氧基烷基或C 3 -C 8链烷氧基烷基取代; A和B各自独立地是氧或硫,或者A和B中的一个是次甲基,X是还可以另外含有氯的氟化的C 1 -C 3烷基,Y是氢,C 1 -C 4烷基 ,C 1 -C 4卤代烷基,C 1 -C 4烷氧基,C 1 -C 4卤代烷氧基或苯基。

    Pyrimido-2-benzazepines
    60.
    发明授权
    Pyrimido-2-benzazepines 失效
    嘧啶-2-苯并吖庚因

    公开(公告)号:US4481142A

    公开(公告)日:1984-11-06

    申请号:US437047

    申请日:1982-10-27

    摘要: There is presented compounds of the formula ##STR1## wherein A is selected from the group consisting of ##STR2## R.sub.1 is selected from the group consisting of hydrogen, chlorine, bromine, lower alkyl, the group NR.sub.4 R.sub.5, the group --CH.sub.2 --CO--R.sub.7, the group--NH(CH.sub.2).sub.m NR.sub.8 R.sub.9, hydroxy, lower alkoxy, mercapto and lower alkyl mercapto; R.sub.2 is selected from the group consisting of hydrogen, amino and dilower alkyl amino; R.sub.3 is selected from the group consisting of hydrogen, lower acyloxy and hydroxy; X is selected from the group consisting of hydrogen, halogen, trifluoromethyl, ethyl, .alpha.-hydroxy ethyl and acetyl; Y is hydrogen or halogen; R.sub.4 and R.sub.5 are hydrogen or lower alkyl or together with their co-bonded nitrogen atom form a five to seven membered heterocyclic group; R.sub.7 is selected from the group consisting of hydroxy lower alkoxy and NR.sub.8 R.sub.9 ; R.sub.8 and R.sub.9 are hydrogen or lower alkyl; n is 0 or 1 and m is 1 to 7 with the limitations that (1) at least one of R.sub.1 and R.sub.2 are hydrogen, (2) when R.sub.3 is lower acyloxy or hydroxy, A is the group (a), X is hydrogen, halogen, trifluoromethyl, ethyl or acetyl and R.sub.1 is the group --NH(CH.sub.2).sub.m NR.sub.8 R.sub.9, then R.sub.8 and R.sub.9 are lower alkyl, (3) when A is group (d) and R.sub.1 is the group --NH(CH.sub.2).sub.m NR.sub.8 R.sub.9 then R.sub.8 and R.sub.9 are lower alkyl and (4) when n is 1, R.sub.1 is hydrogen, lower alkyl, lower alkoxy, chlorine, bromine or the group --CH.sub.2 --CO-- R.sub.7 with R.sub.7 as above then A is the group (a) or (b) and the pharmaceutically acceptable salts thereof.The compounds exhibit pharmacological activity as anxiolytics and sedatives.Also presented Are various novel intermediates and processes to produce the above end products.

    摘要翻译: 提供式IMA的化合物,其中A选自由下列组成的组:R 1选自氢,氯,溴,低级烷基,NR 4 R 5基团,基团 -CH 2 -CO-R 7,基团-NH(CH 2)m NR 8 R 9,羟基,低级烷氧基,巯基和低级烷基巯基; R2选自氢,氨基和二元烷基氨基; R3选自氢,低级酰氧基和羟基; X选自氢,卤素,三氟甲基,乙基,α-羟基乙基和乙酰基; Y是氢或卤素; R4和R5是氢或低级烷基,或与它们的共键键合的氮原子一起形成5至7元杂环基; R7选自羟基低级烷氧基和NR8R9; R8和R9是氢或低级烷基; n为0或1,m为1至7,限制为(1)R 1和R 2中的至少一个为氢,(2)当R3为酰氧基或羟基时,A为(a),X为氢 ,卤素,三氟甲基,乙基或乙酰基,R 1为基团-NH(CH 2)m NR 8 R 9,则R 8和R 9为低级烷基,(3)当A为基团(d)且R 1为基团-NH(CH 2)m NR 8 R 9时 R8和R9为低级烷基,(4)当n为1时,R1为氢,低级烷基,低级烷氧基,氯,溴或基团-CH2-CO- R7,R7为上述,则A为(a)或 (b)及其药学上可接受的盐。 该化合物显示出作为抗焦虑药和镇静剂的药理活性。 还提出了各种新型中间体和方法来生产上述最终产品。