- Synthesis method of 4-ethynyl-tetrahydropyran or 4-ethynyl piperidine
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The invention relates to the technical field of organic synthesis. For solving the problems that a conventional synthesis method of 4-ethynyl-tetrahydropyran and 4-ethynyl piperidine is complex in operation, high in cost and unsuitable for industrial production in the prior art, the invention provides a synthesis method of 4-ethynyl-tetrahydropyran or 4-ethynyl piperidine, wherein the synthesis method comprises the following steps: carrying out Wittig reaction on carbonyl of a compound represented by the formula (I) and phosphorus ylide salt under the action of a strong alkali to generate a compound represented by the formula (II), wherein the reaction temperature is 0-50 DEG C; (2) hydrolyzing the compound represented by the formula (II) to generate a compound represented by the formula (III), wherein the reaction temperature is 20-60 DEG C; (3) carrying out a Corey-Fuchs reaction on the compound represented by the formula (III) to obtain a compound represented by the formula (IV), wherein the reaction temperature is -20 to 40 DEG C; and (4) carrying out a reaction of the compound represented by the formula (IV) with a strong alkali, and carrying out a reaction with a silica reagent to generate a compound represented by the formula (V), wherein the reaction temperature is -70 to 20 DEG C. The method has the advantages of simple and accessible raw materials, low cost, simple synthesis steps and high yield, and is suitable for laboratory small-scale preparation and industrial production.
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Paragraph 0023
(2020/01/12)
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- Therapeutic agent for overactive bladder involved in aging
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A method for treating overactive bladder involved in aging, comprising administrating a compound having a cholinesterase inhibitory activity, a pharmacologically acceptable salt or a solvate thereof to a patient with the overactive bladder involved in aging.
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Page/Page column 18
(2010/11/08)
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- Indole and indazole derivatives, for the treatment and prophylaxis of cerebral disorders, their preparation and their use
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Compounds of formula (I) : [in which R1 and R2 are each hydrogen or various organic groups, pis 0, 1, 2 or 3, U is -CO- or -CH(OR3)- where R3 is hydrogen or a hydroxy-protecting group, V is an optionally unsaturated aliphatic hydrocarbon group and W is a nitrogen-containing group] are useful in the treatment and prophylaxis of dementia especially of the Alzheimer's type.
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- N-ARALKYL PIPERIDINE DERIVATIVES AS PSYCHOTROPIC DRUGS
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There are provided N-aralkyl piperidine derivatives which are selective sigma receptor antagonists. These compounds and pharmaceutical compositions containing them are useful for treating physiological or drug induced psychosis or dyskinesia in a mammal.
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