39 results about "Protuberic acid" patented technology

Novel solution complexes of zoledronic acid are described which give rise to improved properties of zoledronic acid. The invention includes aqueous solution and molecular complexes of zoledronic acid with and optical isomers of asparagine, histidine, arginine and proline as well as pharmaceutical complexes containing them and methods of treatment using them.

The invention discloses a tetrahydroindole compound, and a preparation method and an application thereof, and belongs to the technical field of the chemical synthesis. Raw materials comprising a 1,3-cyclohexanedione compound, nitroalkene and amine undergo a one-pot process under microwave radiation in water as a solvent under the action of L-proline as a catalyst to prepare the tetrahydroindole compound in high yield. The catalyst used in the invention is a non-transition metal catalyst having a low price, so the synthesis cost is substantially reduced; the reaction condition in a catalysis system is mild and can be easily controlled, and the product can be obtained through a domino cyclized multi-component one-step reaction; and the method has the advantages of green and pollution-free experiment program, simple and effective experiment operation, and diversified product structure. The method which uses water as a solvent has the characteristics of simple post-treatment, small pollution to the environment, no damages to the health of the body of an operation worker, and easy realization of the industrialized production.

The invention relates to compounds of general formula (I), which can be used particularly as structural mimetics of proline-rich peptides and are therefore capable of binding PRM binding domains (proline-rich motif binding domains) of proteins. The invention also relates to the use of said compounds as pharmaceutical active agents and the use of these pharmaceutical active agents for treating bacterial diseases, neurodegenerative diseases and tumors.

The invention provides a method for preparing zofenopril calcium. N-acetyl-L-oxyproline is adopted as a raw material. The method includes: a step of subjecting the N-acetyl-L-oxyproline and methanol to esterification, subjecting the obtained product and paratoluensulfonyl chloride to sulfonation, and subjecting the obtained product and thiophenol prepared from a sodium thiophenolate solution to thiophenyl substitution; a step of hydrolyzing the obtained product into an free acid by utilization of an alkali, performing recrystallization for purification, and performing deacetylation with hydrochloric acid to obtain (cis)-4-thiophenyl-L-proline hydrochloride; a step of reacting (S)-3-(benzoyl sulfhydryl)-2-methylpropanoic acid with thionyl chloride to obtain (S)-3-(benzoyl sulfhydryl)-2-methyl propionylchloride; a step of reacting the (S)-3-(benzoyl sulfhydryl)-2-methyl propionylchloride with the (cis)-4-thiophenyl-L-proline hydrochloride to obtain the free acid zofenopril; and a step of forming a potassium salt, purifying and reacting with a calcium chloride to obtain a calcium salt, thus obtaining a final product zofenopril calcium. The method has characteristics of easily available raw materials, simple preparation method, mild conditions, easy control, reasonable monitoring points in the preparation process, effective removal and control of impurities, capability of producing the final product with the needed crystal form preferentially in a high ratio, suitability for industrial production and large application value.

The invention discloses a synthetic method of an oxidation indoles compound. The synthetic method comprises the following steps of: taking an anilines compound as a raw material to generate an adjacent bromaniline compound; getting cuprous iodide as a catalyst and getting L-proline and inorganic salt cesium carbonate as additives to conveniently achieve an arylation coupling reaction between molecules of a bromoaniline compound and a beta-dicarbonyl compound; and finally carrying out intramolecular cyclization so as to further synthesize the oxoindole compound. According to the synthetic method disclosed by the invention, selected raw materials are easy to obtain; the catalyst and ligands are cheap; a reaction condition is mild; and the most important is that a simple recrystallizing method is adopted during post-purifying processing of a product; the synthetic method has the advantages of being simple and convenient to operate, and high in chemical yield and the like, and is more suitable for industrial production, and has a good application prospect; and another new way and method are provided for synthesizing and purifying the oxoindole compound.

The invention relates to a methylbenzene recycling method applied to a sulfosalicylic acid method for determination of proline contents inside plants. The purpose of the invention is to solve the technical problems that a large amount of methylbenzene waste liquor is produced in the sulfosalicylic acid method for determination of proline contents inside plants, the direct pouring of the waste liquor results in serious pollution to the environment and the testing cost is high. The recycling method comprises a decoloring step and a filtering step. The recycling method has the advantages of reducing the pollution of the methylbenzene waste liquor in the sulfosalicylic acid method for determination of proline contents inside plants to the environment, improving the utilization rate of organic solvent and reducing the testing cost, and has the characteristics of being simple in operation, high in processing capacity and easy in manual control and the like; the recycling method has certain application value to the physiological characteristics of plants; the methylbenzene recovery rate is 85%; the recycling times of active carbon is eight; and the recycling method is applicable to treatment of a large amount of samples.