Abstract:
There is disclosed a process comprising reacting a compound having the general structural Formula II: ##STR1## with a compound having the general Formula III: ##STR2## in the presence of a basic catalyst while dissolved in an organic solvent to yield an aldehyde having the structural Formula I: ##STR3## wherein R.sub.1 and R.sub.2 are the same or different radicals selected from the group consisting of tertiary alkyl radicals having from 4 to 12 carbon atoms, R.sub.3 and R.sub.4 are the same or different radicals selected from the group consisting of alkyl radicals containing from 1 to 12 carbon atoms, cycloalkyl radicals containing from 5 to 12 carbon atoms, phenyl and substituted phenyl radicals or R.sub.3 and R.sub.4 with the carbon atom to which they are joined may form a cycloalkyl ring of from 5 to 12 carbon atoms, R.sub.5 is selected from the group consisting of hydrogen, alkyl radicals containing from 1 to 12 carbon atoms, or a cycloalkyl radical containing 5 or 6 carbon atoms.
Abstract:
Anti-inflammatory compositions are prepared which comprise a therapeutically effective effective amount of a compound of the formula ##STR1## wherein X is CO; Y is an oxygen atom; the dotted line represents a double bond which is present or absent; R.sub.1 is hydrogen or methyl; R.sub.2 is hydrogen; and R.sub.3 is phenyl unsubstituted or substituted by 1 or 2 substituents selected from the group consisting of fluorine, chlorine, bromine, methyl, ethyl, methoxyl, ethoxyl, benzyloxyl, hydroxyl, acetoxyl, trifluoromethyl, nitro, amino, acetyl, methylthiol, methylsulphonyl, methylamino and dimethylamino; in combination with a pharmaceutically acceptable carrier. Methods of treating inflammation utilizing the compounds of formula (I) are part of the present invention together with the compounds themselves of the above formula.
Abstract:
Aryl substituted diketones and keto-esters, useful as antiviral agents and insecticides, are prepared by reacting an arylalkyl or arylalkenyl iodide with a metal salt of the appropriate diketone or keto-ester.
Abstract:
Aryl substituted diketones and keto-esters, useful as antiviral agents and insecticides, are prepared by reacting an arylalkyl or arylalkenyl iodide with a metal salt of the appropriate diketone or keto-ester. The intermediate iodides are prepared by condensing a methyl cyclopropyl ketone with an aromatic aldehyde to give an arylvinyl cyclopropyl ketone, reducing the latter to an arylethyl cyclopropyl carbinol or arylvinyl cyclopropyl carbinol, treating the carbinol with phosphorus tribromide and then with zinc bromide to give an arylalkyl or arylalkenyl bromide, and then replacing the bromine atom by iodine.
Abstract:
Beta-diketones substituted by an aryl-aliphatic group in which the aliphatic chain is interrupted by a cyclic group, and useful as anti-viral agents, are prepared by interacting the appropriate aryl-aliphatic halide with an alkali metal salt of a beta-diketone.
Abstract:
3,5-Di-tert alkyl-4-hydroxybenzylpyridinium salts are reacted under basic conditions with compounds containing active methylene groups to form phenolic antioxidants. For example, 3,5-di-tert.butyl-4-hydroxybenzylpyridinium chloride is reacted with 2-nitropropane to produce 1,1-dimethyl-2-(3,5-di tert.butyl-4-hydroxyphenyl)-1-nitroethane.
Abstract:
The invention relates to the manufacture of compounds of the formula in which R1 is a secondary or tertiary alkyl group, R2 is an alkyl group, R13 and R14, which may be the same or different, are hydrogen atoms or alkyl, aryl, alkaryl, aralkyl or carbalkoxy groups and R15 is a hydrogen atom, an alkoxy, alkylthioalkyloxy, amino, alkylamino, dialkylamino, alkyl, aryl, alkaryl or aralkyl group or a group in which Z is a straight or branched alkylene group. The compounds are made by additive reaction an appropriate 2,6-dialkylphenol and an unsaturated compound of the formula CH(R13)=C(R14)COR15, the reaction being effected in the presence of a basic catalyst, e.g. a quaternary ammonium base, an alkali-metal amide, alkoxide or hydroxide or an alkaline-earth metal alkoxide or hydroxide, and optionally in a solvent, e.g. a tertiary alkanol, tetrahydrofuran, dimethyl formamide or acetone. The reaction may be effected at 25-200 DEG C. at atmospheric or raised pressure. Examples are given in which (1) 2,6-di-tert.-butylphenol and methyl acrylate yield methyl (3.5-di-tert.-butyl - 4 - hydroxyphenyl) propionate, (2) 2.6-di-tert.-butylphenol and lauryl (or octadecyl) acrylate yield dodecyl (or octadecyl) 3,5 - di - tert. - butyl - 4 - hydroxyphenyl) propionate, (3) 2,6 - di - tert. - butylphenol and diethyl maleate yield diethyl (3,5-di-tert.-butyl - 4 - hydroxyphenyl) succinate, (4) 2.6-di - tert. - butylphenol and acrylamide yield 3,5 - di - tert. - butyl - 4 - hydroxyphenyl propionamide, (5) 2.6 - di - tert. - butylphenol and N - octadecyl acrylamide yield N - octadecyl-3,5 - di - tert. - butyl - 4 - hydroxyphenyl propionamide, (6) 2.6 - di - tert. - butylphenol and methyl vinyl ketone yield 4-(3.5-di-tert.-butyl-4 - hydroxyphenyl) butan - 2 - one, and (7) 2.6 - di - tert. - butylphenol and ethylene bis-acrylate yield ethylene bis(3,5 - di - tert. - butyl - 4 - hydroxyphenyl) propionate. Other specified phenols are 6-tert.-butyl-o-cresol, 6-(1,1,3,3 - tetramethylbutyl) - o - cresol, 2 - sec.-butyl - 6 - tert. - butylphenol, 2,6 - bis(1,1 - dimethyl - n - propyl)phenol and 2.6 - bis(1-methyl - n - nonyl)phenol. Other alkyl groups which may constitute or form part of the radicals R1, R2, R13, R14 and R15 in the first formula above are specified, and it is stated that R13, R14 and R15 may also be naphthyl or acenaphthyl groups. The products are useful as stabilizing agents for hydrocarbon polymers, e.g. polyethylene or polypropylene, waxes, soaps, greases, natural and synthetic rubbers and animal, vegetable or mineral oils, including lubricating oils, fuel oils and gasoline. Specification 965,373 is referred to.ALSO:As stabilizing agents for hydrocarbon polymers, e.g polyethylene or polypropylene, and for natural and synthetic rubbers, use is made of compounds of the formula in which R1 is a secondary or tertiary alkyl group, R2 is an alkyl group, R13 and R14, which may be the same or different, are hydrogen atoms or alkyl, aryl, alkaryl, aralkyl or carbalkoxy groups and R15 is a hydrogen atom, am alkoxy, alkylthioalkyloxy, amino, alkylamino, dialkylamino, alkyl, aryl, alkaryl or aralkyl group or a group in which Z is a straight or branched alkylene group (see Division C2). Typical compounds are methyl (3,5 - di - tert - butyl - 4 - hydroxyphenyl) propionate, dodecyl (or octadecyl) (3,5 - di - tert. - butyl - 4 - hydroxyphenyl) propionate, diethyl (3,5 - di - tert. - butyl - 4 - hydroxyphenyl) succinate, 3,5 - di - tert. - butyl - 4 - hydroxyphenyl propionamide, N - octadecyl - 3,5 - di - tert. - butyl - 4 - hydroxyphenyl propionamide, 4 - (3,5 - di - tert. - butyl - 4 - hydroxyphenyl) butan-2-one, and ethylene bis-(3,5 - di - tert. - butyl - 4 hydroxyphenyl) propionate. Specification 965,373 is referred to.ALSO:As stabilizing agents for waxes, soaps, greases and vegetable and mineral oils, including lubricating oils, fuel oils, and gasolene, use is made of compounds of the formula in which R1 is a secondary or tertiary alkyl group, R2 is an alkyl group, R13 and R14, which may be the same or different, are hydrogen atoms or alkyl, aryl, alkaryl, aralkyl or carbalkoxy groups and R15 is a hydrogen atom, an alkoxy, alkylthioalkyloxy, amino, alkylamino, dialkylamino, alkyl, aryl, alkaryl or aralkyl group or a group in which Z is a straight or branched alkylene group (see Division C2). Typical compounds are methyl (3,5 - di - tert. - butyl - 4 - hydroxyphenyl) propionate, dodecyl (or octadecyl) (3,5-di - tert. - butyl - 4 - hydroxyphenyl) propionate, diethyl (3,5 - di - tert. - butyl - 4 - hydroxyphenyl) succinate, 3,5-di-tert.-butyl-4-hydroxyphenyl propionamide, N-octadecyl-3,5-di-tert.-butyl-4-hydroxyphenyl propionamide, 4-(3,5-di - tert. - butyl - 4 - hydroxyphenyl) butan - 2 - one and ethylene bis(3,5-di-tert.-butyl-4-hydroxyphenyl) propionate. Specification 965,373 is referred to.
Abstract:
The present invention relates to a sacubitril intermediate and a preparation method thereof. The sacubitril intermediate disclosed herein can be prepared by a deprotection reaction of a compound. In addition, the intermediate can be used as a raw material to synthesize sacubitril.