摘要:
A new process for the production of salts of 1,3-dioxolane-4-carboxylic acid corresponding to the following formula ##STR1## using as a starting material an isomer mixture of a 4-hydroxymethyl-1,3-dioxolane and a 5-hydroxy-1,3-dioxane obtained by reacting glycerin with an aldehyde or ketone having the formula R.sup.1 R.sup.2 CO. The 4-hydroxymethyl-1,3-dioxolane may be selectively oxidized from the isomer mixture in the presence of a platinum metal catalyst at an alkaline pH. The unreacted 5-hydroxy-1,3-dioxane may be extracted from the reaction mixture and the 1,3-dioxolane-4-carboxylic acid salt isolated in pure form.
摘要:
Derivatives of 2-substituted-cycloheptoimidazole are disclosed, which are represented by the following formula: ##STR1## wherein R is a hydrogen atom, a lower-alkyl, acetyl, lower-alkylaminoalkyl or ethylenedioxyethyl group. A represents a phenyl, pyridyl, benzimidazolyl, imidazolyl, thiazolyl, thiadiazolyl, oxazolyl or isoxazolyl group; each of which optionally possesses one substituent or more and m is 0 or 1, and n is 1 or 2. These compounds are useful as anti-ulcerative agents.
摘要:
Novel antibacterially active 1-cyclopropyl-1,4-dihydro-4-oxo-7-[4-(2-oxo-1,3-dioxol-4-yl-methyl)-1-piperazinyl]-3-quinolinecarboxyic acids of the formula in which ##STR1## R is hydrogen or, together with R.sup.1, forms an alkylene radical with 2 or 3 carbon atoms,R.sup.1 is hydrogen, alkyl with 1 to 4 carbon atom or phenyl,R.sup.2 and R.sup.3 each independently is hydrogen, methyl, ethyl, cyclohexyl, methylene-dioxphenyl, furyl, tetrahydrofuryl or thienyl; or phenyl which is optionally mono-, di or tri-substituted by fluorine, chlorine, bromine, methyl, phenyl, cyano, hydroxyl, ethoxy, benzyloxy, amino, methylamino, dimethylamino, piperidino or nitro,X.sup.1 is hydrogen, halogen, or nitro, andX.sup.2 is hydrogen or halogen,or pharmaceutically acceptable hydrates, acid addition salts, alkali metal salts or alkaline earth metal salts thereof.
摘要:
Substituted isoxazolidines of the formula ##STR1## in which R.sup.1 represents optionally substituted alkyl, cycloalkyl, aralkyl, aryl or heteroaryl or radicals of the formula --COR.sup.4,R.sup.4 represents optionally substituted alkyl, aryl, alkoxy, alkylthio, aroxy, arylthio, amino, alkylamino, dialkylamino, arylamino, arylalkylamino, diarylamino or cycloalkylamino, or optionally substituted heterocyclic radicals which are bonded via nitrogen,R.sup.2 represents hydrogen or the radicals mentioned for R.sup.1, it being possible for R.sup.1 and R.sup.2 to be identical or different, andR.sup.3 represents optionally substituted alkyl, cycloalkyl, alkenyl, alkinyl or aryl, or saturated heterocyclic radicals, which are optionally substituted,and acid salts thereof, are pesticidally active and increase animals' utilization of feed. Intermediates therefor are also new.
摘要:
The invention relates to novel decahydroquinolinol derivatives represented by the general formula: ##STR1## and pharmaceutically acceptable acid addition salts thereof, in which X represents oxygen or sulphur, R represents an alkyl radical having from 1 to 3 carbon atoms, R.sub.1 represents fluorine, chlorine, bromine or methoxy, R.sub.2 represents hydrogen or methoxy or R.sub.1 and R.sub.2, when they are taken together, represent a 2,3-methylenedioxy or 3,4-methylenedioxy radical.The compounds of the invention are inhibitors of calcium translocation at the level of the cell membrane and are useful more particularly in the treatment of pathological syndromes of the cardiovascular system such as, for instance, angina pectoris.
摘要:
There are disclosed pyridine-2-ethers and pyridine-2-thioethers having a nitrogen-containing cycloaliphatic ring corresponding to the formula ##STR1## the pyridine-N-oxides and/or amine oxides thereof and the pharmaceutically acceptable salts thereof. The compounds show analgesic activity.
摘要:
Compounds of formula (I): ##STR1## wherein: A represents a CH-NO.sub.2 group or a N-CN group;B represents CH.sub.2, O, S or a direct bond;R represents a bicyclic or polycyclic residue, variously substituted and functionalized;R.sup.1 and R.sup.2, which may be the same or different, are hydrogen or C.sub.1 -C.sub.4 alkyl groups; andn and m, which may be the same or different, are 0, 1, 2, 3 or 4;are valuable pharmacological agents.
摘要:
There is disclosed herewith a method of producing morphinan compounds by total synthesis which incorporates utilization of N-cycloalkylcarbonyl compounds, which show certain advantages over the prior art which has been previously expressed in U.S. Pat. No. 4,368,326.
摘要:
Pyridoindoles of the formula ##STR1## in which R.sub.1 represents hydrogen or C.sub.1 -C.sub.4 -alkyl, which is optionally substituted by the radical ##STR2## R.sub.2 and R.sub.3 represent H or form a bond, or R.sub.1 and R.sub.2 together represent O, --O--CH.sub.2 --CH.sub.2 --O-- or --S--CH.sub.2 --CH.sub.2 --S--,R.sub.4 represents H or the ##STR3## or R.sub.3 and R.sub.4 represent O, orR.sub.1 and R.sub.4 are members of an N-containing six-membered ring andR.sub.8 and R.sub.9 represent H or C.sub.1 -C.sub.4 -alkyl, or optionally form, with the N atom, a heterocyclic 5-membered or 6-membered ring, which can optionally also contain a further hetero-atom from the series comprising N, O or S,R.sub.5 represents H, C.sub.1 -C.sub.4 -alkyl or the group ##STR4## or R.sub.5 and R.sub.3 form a bond, andR.sub.10 and R.sub.11 represent C.sub.1 -C.sub.4 -alkyl or are members of an N-containing 5-membered or 6-membered ring,R.sub.6 represents H or C.sub.1 -C.sub.4 -alkyl andR.sub.7 represents halogen,or acid addition salts thereof, which are active on the central nervous system. Novel intermediates are also shown.
摘要:
Perfluoro-1,3-dioxole, prepared by dechlorinating 4,5-dichloro-2,2,4,5-tetrafluoro-1,3-dioxolane with magnesium, is a useful monomer, which polymerizes to either amorphous or liquid homopolymers and copolymerizes with tetrafluoroethylene as well as with other monomers to both crystalline and amorphous copolymers having one or more such comonomers incorporated therein. Amorphous homopolymers and copolymers of perfluoro-1,3-dioxole are useful in such applications as glazing for reactors for hydrogen fluoride reactions. Amorphous homopolymers and amorphous or crystalline copolymers form self-supporting films and can be used for coatings and linings which are inert to most chemicals and are stain and weather resistant and as dielectrics for electrical and electronic equipment. Liquid homopolymers can be used as hydraulic fluids and heat exchange media.