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.
摘要:
11-Haloprostane derivatives of general formula I ##STR1## wherein X is F, Cl or Br,R.sub.1 is the residue CH.sub.2 OH or ##STR2## wherein R.sub.2 means a hydrogen atom, an alkyl, cycloalkyl, aryl, phenacyl or heterocyclic residue,A is a --CH.sub.2 --CH.sub.2 -- or cis-CH.dbd.CH-group,B is a --CH.sub.2 --CH.sub.2 -- or trans-CH.dbd.CH-- or a --C.tbd.C-group,W is an ethylenedioxymethylene group or a hydroxymethylene group,D and E together mean a direct bond orD is a C.sub.1-10 -alkylene group,E is an oxygen or sulfur atom, a direct bond, a --C.tbd.C-bond or a --CR.sub.6 .dbd.CR.sub.7 -group with R.sub.6 and R.sub.7 meaning a hydrogen atom, a chlorine atom or an alkyl group,R.sub.4 is a hydroxy group,R.sub.5 is a hydrogen atom, an alkyl, a cycloalkyl, an aryl or a heterocyclic group, andthe salts thereof with physiologically compatible bases, processes for their preparation, and use thereof as agents inhibiting gastric acid secretion.
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:
The new compound ##STR1## is prepared and converted to the new acetal ##STR2## which is reacted with an alkali phenolate or alkaline earth metal phenolate in the presence of copper or a copper compound as a catalyst and in the presence of a diluent at a temperature between about 100.degree. and 200.degree. C. to produce the new acetal ##STR3## which can be hydrolyzed to the corresponding aldehyde which is a known intermediate for pyrethroid-like insecticides.
摘要:
Process for preparing esters of alkanoic acids via rearrangement of alpha-haloketals in the presence of a Lewis acid.The rection is preferably carried out in the presence of catalytic amounts of a Lewis acid and of a diluent at a temperature in the range from about 0.degree. to the reflux temperature of diluent.The esters thus obtained are useful as intermediate products for preparing drugs.The process involves the preparation of new alpha-haloketals.
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:
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:
Compounds of the formula ##STR1## wherein ring B stands for 1,4-phenylene or a trans-1,4-disubstituted cyclohexane ring and A stands for a group with 1 to 3 six-membered rings, which together with ring B represents a central group of formulae II-XIII; R.sup.1 signifies a straight-chain alkyl group containing 1 to 9 carbon atoms or when R.sup.1 is attached to a benzene, monofluorinated benzene or pyrimidine, ring R.sup.1 also signifies a straight-chain alkoxy group with 1 to 9 carbon atoms; and R.sup.2 signifies hydrogen, cyano or a straight-chain alkyl group containing 1 to 7 carbon atoms,their manufacture, liquid crystalline mixtures which contain said compounds and their use for electro-optical purposes are described.The compounds of formula I are especially valuable as components in liquid crystal mixtures and for the most part themselves have liquid crystalline properties.
摘要:
Substituted aminoketals of the formula ##STR1## in which R.sup.1 to R.sup.4 are various organic radicals andR.sup.2 may also be hydrogen,are fungicidally active. Some of the compounds are new.
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。