40 results about "Methylenedioxy" patented technology

The present invention provides R-3,4-methylenedioxy-N,N-dimethylamphetamine, and salts thereof, for treating brain disorders.

The present invention relates to use of a multifunctional isoquinoline ligand, namely 1-(7-amino-4,5,6-triethoxy-1-oxo-1,3-dihydro-3-isobenzofuran)-8-methoxy-2-methyl-6,7-methylenedioxy-2,3,4-tetrahydroisoquinoline or tritoquinoline, for treating dry eye, meibomian gland dysfunction and lacrimal gland dysfunction.

The present invention is directed to novel chemical compositions of matter, and in particular novel MDMA class of compounds having substituted methylenedioxyphenethylamine and substituted amphetamine, having a metabolically labile thioether group.

The invention relates to the technical field of organic synthesis, and provides a preparation method of 3-methoxy-4, 5-methylenedioxy phenylethylamine. According to the invention, myristic aldehyde and diethyl cyano phosphate are adopted as initial raw materials, and the 3-methoxy-4, 5-methylenedioxy phenylethylamine is prepared through wittig reaction, reduction reaction, hydrolysis reaction and Hofmann reaction. According to the preparation method provided by the invention, each step is simple and convenient to operate, the product yield is high (the total yield is 78.3%-84.2%), and the purity is high; furthermore, the preparation method provided by the invention is mild in reaction condition, does not need explosive and highly toxic chemicals, does not need column chromatography purification of products in each step, and is suitable for industrial production.

The application discloses a synthesis process of (-)-alpha-lycorane alkaloid and belongs to the technical field of organic synthesis chemistry. (2Z,4E)-7,7-diethoxy-3-hydroxyhepta-2,4-dienoic acid methyl ester and 3,4-methylenedioxy-beta-nitrostyrene are used as starting materials, and (-)-alpha-lycorane is obtained through catalytic asymmetric tandem Michael addition reaction, nitro reduction amination reaction, Boc amidation reaction, Bischler-Napieralski cyclization reaction, ketone enolization tandem esterification reaction, enol triflate reductive hydrogenolysis reaction and amide reduction reaction in sequence. (-)-Alpha-lycorane has a four-membered ring core skeleton of pyrrole-phenanthridine ring, has good in-vitro tumor inhibition activity and cell proliferation growth inhibition activity. The synthesis process can realize efficient, simple and full synthesis of (-)-alpha-lycorane.

This invention provides an ether-based electrolyte for improving the high-voltage and long-cycle stability of sodium-ion batteries, its preparation method, and its application. The ether-based electrolyte comprises a base electrolyte and additives; the additives include aromatic isocyanates and alkoxysilanes. The aromatic isocyanates are a combination of one of the following: 6-fluoro-1H-1,3-benzodioxane-8-yl isocyanate, 3,4-dihydro-1,5-benzodioxane-7-isocyanate, or 3,4-(methylenedioxy)phenyl isocyanate, and 4-trifluoromethoxyphenyl isocyanate; the alkoxysilanes are 2-cyanoethyltriethoxysilane or 3,3,3-trifluoropropyltriethoxysilane. The electrolyte of this invention achieves synergistic regulation of interfacial reactions and interfacial film evolution, is suitable for sodium-ion half-cells or full-cells, and can improve overall stability and operating efficiency under high-voltage and long-cycle operating conditions.

The invention provides an electrochemical preparation method of heliotropin, which comprises the following steps: 1) mixing 3, 4-(methylenedioxy) toluene, an alcohol solvent, water, halide and a sulfonate anionic surfactant to obtain an electrolyte, and adding the electrolyte into an electrolytic bath; and 2) electrifying the electrolyte in the electrolytic bath in the step 1) to react, and generating heliotropin at an anode by using 3, 4-(methylenedioxy) toluene and an alcohol solvent. The method has the advantages of high reaction yield, high atom economy, simple steps, less three wastes, low energy consumption and low cost.

The application belongs to the field of organic chemistry and particularly relates to a synthesis method of berberine hydrochloride. The method comprises the following steps: taking 3,4-dimethoxyphenethylamine hydrochloride and 3,4-methylenedioxybenzaldehyde as starting materials, sequentially undergoing oxidative cyclization, selective reduction and quaternary ammonium ring closure through three-step reactions, and finally directly obtaining the target product berberine hydrochloride through acid treatment. The technical scheme has the characteristics of high efficiency, simplicity, and high industrial cost ratio in the synthesis of berberine hydrochloride, the overall reaction is more green and safe, the reaction condition is more mild, the reaction process has high selectivity, and the berberine hydrochloride product with higher purity can be obtained.

The application belongs to the field of biological medicine, and discloses a 2-methyl quinoline derivative with a structure as shown in formula I, R is selected from substituted phenyl as shown in the formula, n is an integer of 1-5, R1 is selected from C1-C3 alkyl, halogen-substituted C1-C3 alkyl, C1-C3 alkoxy, halogen-substituted C1-C3 alkoxy, 3,4-methylenedioxy, phenyl and -NR3R4; R3 and R4 are independently selected from H and C1-C3 alkyl; however, the substituted phenyl does not include p-methoxyphenyl and 3-amino-4-methoxyphenyl; X is selected from C and N, and R2 is selected from H and C1-C3 alkyl, but X cannot be selected from C and R2 cannot be selected from H at the same time. The 2-methyl quinoline derivative has good antitumor activity, and the toxicity to human normal cells is weaker than the toxicity to cancer cells. The application discloses application of the 2-methyl quinoline derivative in preparation of an antitumor drug.

The present invention provides a 12-substituted camptothecin derivative and its uses, belonging to the technical field of medicine. The 12-substituted camptothecin derivative provided by the present invention, or its stereoisomers and pharmaceutically acceptable salts, has the structure shown in formula (I). By introducing a methylenedioxy group at the 10,11-positions and different substituents at the 12-position on the basis of the traditional camptothecin structure, camptothecin derivatives with excellent anti-tumor activity can be obtained. The obtained 12-substituted camptothecin derivative has clear structural characteristics, is convenient to synthesize, and the purification method is simple and fast. It can be used to prepare drugs for preventing or treating cancer and has broad application prospects.

The present application relates to the field of chemical pharmacy, and particularly relates to a preparation method of sertindole, comprising the following steps: taking 1-bromo-3,4-(methylenedioxy) benzene (compound A) and 4,4-dimethyl-1-penten-3-one (compound B) as raw materials, reacting the compound A with zinc powder to obtain an organic zinc reagent, and reacting the compound B with a chloro reagent to obtain a chloro compound with a terminal olefin substituted; then, the organic zinc reagent of the compound A and the chloro compound of the compound B are coupled to obtain an intermediate compound C; finally, the compound C is reduced to obtain sertindole.

The application belongs to the technical field of organic synthesis and medicine, and particularly relates to 20(S)-10,11-difluoromethylenedioxy camptothecin derivatives, a preparation method and application thereof. The derivative is a compound with a structure shown in formula (I), stereoisomers and pharmaceutically acceptable salt forms. The novel 20(S)-10,11-difluoromethylenedioxy camptothecin derivative can be used for preparing and synthesizing camptothecin drugs for preventing or treating tumors. The compound has good anti-inflammatory activity, in-vivo and in-vitro anti-tumor activity and cell transmembrane transport capacity. The preparation method is easy to operate, the post-treatment is simple, the reaction starting material is cheap and easy to obtain, the reaction substrate has strong designability, the reaction efficiency is high, and the practicability is strong.

The invention discloses application of a compound shown in a formula I or a salt or a deuterated substance thereof in preparation of a 5 alpha-reductase inhibitor, in which ring A is a single benzene ring, a single methylenedioxy benzene ring, or a single five-membered ring containing O or S; wherein the ring A may be substituted by m Ra, and m is 0, 1, 2, 3 or 4; wherein Ra is hydroxyl, methyl, halogen, methoxyl or nitro; wherein the deuterated substance is a partial deuterated substance and / or a perdeuterated substance. In a 5AR activity inhibition experiment, the compound provided by the invention has an obvious inhibition effect: under the concentration of 250 mu M, the 5AR activity inhibition rate (the final administration concentration of 250 mu M) of the aromatic methyleneacetone active small molecule compound protected by the invention is 9-56%, and part of the compound approaches or exceeds the inhibition rate (53%) of finasteride of radix scrophulariae. # imgabs0 #

The invention belongs to the technical field of organic synthesis and medicines, and particularly relates to an aminated 20 (S)-10, 11-difluoromethylenedioxy camptothecin derivative as well as a preparation method and application thereof. The derivative is a compound with a structure as shown in a formula (I), and in the formula (I), R is shown in the description; wherein X is an integer from 3 to 10, and n is an integer from 3 to 10; and Z is selected from (amido substitution). The novel aminated 20 (S)-10, 11-difluoromethylenedioxy camptothecin derivative provided by the invention has good in-vivo and in-vitro anti-tumor activity, and can be used for preparing and synthesizing camptothecin drugs for preventing or treating tumors, the preparation method is easy to operate, the post-treatment is simple and convenient, the initial raw materials of the reaction are cheap and easy to obtain, the designability of the reaction substrate is strong, and the method is suitable for industrial production. The reaction efficiency is relatively high, and the practicability is relatively high.

The present application relates to the technical field of biological analysis detection, and particularly relates to cucurbituril derivatives for drug detection, a preparation method and application of the cucurbituril derivatives, a detection probe containing the cucurbituril derivatives, a drug for treating drug acute poisoning, and a method for drug detection. The derivative introduces a functional group of o-cyanobenzaldehyde (CNBA) on the basis of retaining the original supramolecular recognition characteristics of cucurbituril, and the obtained compound can realize efficient covalent capture on the primary amine groups in common drugs and metabolites (such as methyl phenylpropylamine and its metabolites, 3,4-methylenedioxy methyl phenylpropylamine, ketamine and its metabolites, fluoroamine and its metabolites, phenylcyclohexylpiperidine, and casiketone molecules), so as to realize rapid, high-sensitivity and visual detection on the above target objects, and can be used for antagonistic treatment of acute poisoning caused by related drugs and metabolites.

The invention relates to an aporphine-benzylisoquinoline alkaloid dimer as well as a preparation method and application thereof, and belongs to the field of natural medicines and biological medicines. The aporphine-benzylisoquinoline alkaloid dimer has a structural general formula shown in the specification, in the formula, R1, R2, R3, R4, R5, R6, R7 and R8 are independently selected from hydrogen, methoxyl, hydroxyl or two adjacent substituent groups are methylenedioxy, so that a five-membered ring is formed; and R9 is selected from hydrogen, methoxyl or hydroxyl. Six novel aporphine-benzylisoquinoline alkaloid dimers are extracted and separated from roots of thalictrum omeiensis, and through detection, the aporphine-benzylisoquinoline alkaloid dimers have obvious growth inhibition effects on human acute promyelocytic leukemia cells HL-60 and human prostate cancer cells PC-3, and have the prospect of preparing medicines for preventing and treating tumors.

In one aspect, the present disclosure provides a method of synthesis for methylone HCl, with 3,4-methylenedioxypropiophenone (MDP) as the starting material. In another aspect, the present disclosure provides stereoisomers of methylone. In another aspect, the present disclosure provides phenethylamines or cathinones covalently bound to a chemical moiety in a prodrug form. The presently described prodrug form allows slow / sustained / controlled delivery of the parent phenethylamines or cathinones into the blood system in a manner that would increase the duration of therapeutic efficacy.

The present invention is directed to chemical compositions of matter, and in particular a MDMA class of analogs having 1,3-benzothiazoles substituted at the 5 and 6-position with a basic or modified side chain.

The invention relates to medical uses of a compound of general formula (I), (I) or a pharmaceutically acceptable salt thereof, wherein R1 and R2, which can be the same group or a different group, are independently a hydroxy group or a methoxy group or, taken together, a methylenedioxy group, R3 and R4, which can be the same group or a different group, are independently a hydroxy group or a methoxy group, R5 is phenyl group, and R6 is a phenyl group, wherein said phenyl groups are independently optionally substituted, and wherein n is 2, and to pharmaceutical compositions comprising said compound of general formula (I), for use in the treatment of cancer in a human subject, wherein said compound of general formula (I) is administered in a therapeutically effective dose to said human subject. The invention is also related to medical uses of pharmaceutical compositions comprising said compound of general formula (I) or said pharmaceutically acceptable salt thereof.

Described herein are isotopically enriched analogs of methylone (e.g., deuterated analogs of methylone (e.g., (S)-methylone and (R)-methylone) with improved characteristics. Also described herein are salts (such as hydrochloride salt) and solid forms (e.g., crystalline forms) of methylone. Also described herein are stereoisomers (e.g., enantiomers) of methylone. The present disclosure also provides methods of making and methods of use of the methylone or methylone analogs and solid forms of 3,4-methylenedioxy-N-ethylcathinone hydrochloride described herein to treat brain and neurological disorders such as depression.

The invention relates to a preparation method and application of aporphine-protoberberine alkaloid dimers, and belongs to the field of natural medicines and biological medicines. The aporphine-protoberberine alkaloid dimer disclosed by the invention has a structural general formula shown in the specification, in the formula, R1, R2, R3, R5, R6, R7, R8 and R9 are independently selected from hydrogen, methoxyl, hydroxyl or two adjacent substituent groups are methylenedioxy, so that a five-membered ring is formed; r4 is selected from hydrogen, methoxyl or hydroxyl. Six novel aporphine-protoberberine alkaloid dimers are extracted and separated from thalictrum omeiensis roots, and tests show that the aporphine-protoberberine alkaloid dimers have obvious growth inhibition effects on human acute promyelocytic leukemia cells HL-60 and human prostate cancer cells PC-3, can cause HL-60 cell cycle arrest in an S phase, induce HL-60 cell apoptosis, and can be used for preparing the aporphine-protoberberine alkaloid dimers. The compound has a prospect of preparing medicines for preventing and treating tumors.

The invention belongs to the technical field of organic synthesis, and discloses a rapid synthesis method of a beta-amino acid derivative. The method comprises the following steps: by taking an organic solvent as a reaction medium, reacting 3-hexenoic acid with a dioxazolone compound under the action of pinacolborane, a catalyst, silver salt and an alkaline compound to obtain the beta-amino acid derivative, the structure of the beta-amino acid derivative is as shown in formula I, and R is aryl, furyl, aryl-substituted alkenyl or 3, 4-methylenedioxy phenyl; the catalyst is a dichloro (pentamethyl cyclopentadienyl) rhodium (III) dimer; the organic solvent is a fluorine-containing alcohol solvent. The method has the advantages of mild reaction conditions, no need of nitrogen protection, one-step synthesis of the beta-amino acid derivative, and low energy consumption; the method provided by the invention has high chemical selectivity and high product yield. # imgabs0 #

The present invention includes a novel class of MDMA carbamates that can be activated in vivo as prodrugs. The MDMA prodrugs of the invention are enzymatically cleaved in vivo and produce alcohols of low toxicity that are well tolerated and metabolized in humans.

The present invention is directed to novel chemical compositions of matter, and in particular a novel MDMA class of compounds MDMA analogs having 1,3-benzothiazoles substituted at the 5 and 6-position with a MDMA basic or modified side chain.

The invention relates to the technical field of analytical chemistry, and particularly discloses a method for detecting piperonyl chloride related substances. According to the method, the content of 3, 4-(methylenedioxy) toluene, the content of 5-chloromethyl-6-piperazinyl benzo [1, 3] dioxazole and the content of bis-benzo [1, 3] dioxo-5-yl methane in piperonyl chloride are detected by adopting a gas chromatographic method. According to the detection method provided by the invention, the types and the contents of related substances such as 3, 4-(methylenedioxy) toluene, 5-chloromethyl-6-piperazinyl benzo [1, 3] dioxazole and bis-benzo [1, 3] dioxo-5-yl methane existing in piperonyl chloride can be accurately detected at the same time, and the detection method has the advantages of high sensitivity and high sensitivity. The method is high in specificity, low in detection line and quantitation limit, good in linear relation, high in recovery rate, good in repeatability, high in stability, good in durability, simple and rapid to operate and good in detection result accuracy, and data support can be provided for effective quality control of piperonyl chloride in the production process of piperonyl chloride.

The invention discloses a synthesis process of (-)-alpha-lycolane alkaloid, and belongs to the technical field of organic synthetic chemistry. According to the preparation method, (2Z, 4E)-7, 7-diethoxy-3-hydroxyheptyl-2, 4-dienoic acid methyl ester and 3, 4-methylenedioxy-beta-nitrostyrolene are taken as initial raw materials, and the raw materials are subjected to a one-pot reaction so as to obtain the 3, 4-methylenedioxy-beta-nitrostyrolene. According to the method, (-)-alpha-lycolane is obtained through a catalytic asymmetric series Michael addition reaction, a nitro reductive amination reaction, a Boc amidation reaction, a Bischler-Napieralski cyclization reaction, an enolation series esterification reaction of ketone, a reductive hydrogenolysis reaction of enol trifluoromethanesulfonate and an amide reduction reaction in sequence. The (-)-alpha-lycolane has a four-membered ring core skeleton of a pyrrole-phenanthridine ring, and has good in-vitro tumor inhibition activity and cell proliferation and growth inhibition activity. According to the synthesis process disclosed by the invention, efficient and simple total synthesis of the (-)-alpha-lycolane can be realized.