36results about How to "Highly economical steps" patented technology

The invention discloses a novel synthetic method for 3-formyl-imidazole[1,2-a]pyridine and 2-butyl-5-chloro-1H-imidazole-4-carboxaldehyde, and effective application of the method into synthesis of Necopidem and Saripidem. According to the invention, a 3-formyl-imidazole[1,2-a]pyridine system is established by using a cheap and low toxic Cu-catalyed O2 activated intramolecular olefin under dehydrogenation ammoxidation; conditions for the method are mild, reaction substrates are easily available, a catalytic system is simple, operation is simple, tolerance of functional groups is good, and the method is economical and effective and has very important scientific values and realistic significance.

The invention discloses a novel method for synthesizing an indolo[1,2-a]quinoxaline derivative. The novel synthesis method comprises the following steps: adding a palladium catalyst, an indole compound, acyl chloride, an additive, alkali and a solvent into a glass reaction container, carrying out a reaction under stirring at 110-130 DEG C under the protection of argon, and separating and purifyinga crude reaction product so as to obtain an indolo[1,2-a]quinoxaline compound. According to the invention, a coupling reaction of primary amine-guided acyl chloride and an indole derivative is developed; a series of functionalized indolo[1,2-a]quinoxaline derivatives can be constructed through simple operation; and high step economy and atom economy are achieved. In addition, the reaction in thenovel method provided by the invention has the main advantages of simple and easily-available substrate, single selectivity, good functional group tolerance and high yield.

The invention belongs to the technical field of organic synthesis, and discloses a polysubstituted benzothienopyridine compound and a preparation method thereof. The preparation method comprises the steps of dissolving nitrile amino metal salt and alkali in an organic solvent in a reactor, stirring to react at the temperature of 90-130 DEG C, and separating and purifying the reaction product to obtain the polysubstituted benzothienopyridine compound, wherein the reaction formula of the preparation method is shown as a formula (I) in the description. According to the method disclosed by the invention, a series of polysubstituted benzothienopyridine compounds are synthesized by taking simple and readily available 2-methyl-3-alkynyl benzothiophene and nitrile as reaction raw materials. The method has the characteristics of simple and readily available raw materials, convenience in operation, no transition metal, high step economy, high atom economy, wide substrate applicability, good tolerance of functional groups and the like; and part of application research is carried out, and a derivative product of a drug molecule citalopram is synthesized.

The invention belongs to the technical field of organic synthesis, and discloses poly-substituted alkynyl amidine compounds, a preparation method and an application thereof. The preparation method includes adding and dissolving an alkynyl bromide palladium salt catalyst, an additive and alkali in an organic solvent in a reactor, finally, adding isonitrile and stirring the mixture to react at 90-100 DEG C, and separating and purifying the reaction product to obtain the poly-substituted alkynyl amidine compounds, wherein the reaction formula is shown in a formula (I). The method uses simple andeasily available alkynyl bromide, amine and isonitrile as reaction raw materials to synthesize a series of poly-substituted alkynyl amidine compounds. The method has the characteristics of simple andeasily-available raw materials, convenient operation, mild conditions, high step economy, wide substrate applicability, good tolerance of functional groups and the like; and some of application studies of the method are carried out and a variety of useful nitrogen-containing heterocycles are synthesized.

3-aryl-3'-amino bis(quaternary carbon) bis(oxindole) compounds and a synthetic method and applications thereof are disclosed. The compounds are prepared from diazo compounds, N,N-disubstituted anilineand isatin imine compound by adopting rhodium acetate as a catalyst, an organic solvent as a solvent and a 4A molecular sieve as an additive through one-step reaction at room temperature. The methodhas advantages of efficient atom economy, high selectivity, a low dosage of the catalyst, simple and safe operation, and the like. The synthesized bis(quaternary carbon) bis(oxindole) compounds can beadopted as important medical and chemical intermediates and have wide application prospects in the medicinal field.

The invention belongs to the technical field of organic synthesis, and discloses a polysubstituted benzodihydrofuro heterocyclic compound and a preparation method and application thereof. The preparation method comprises the following steps: adding a palladium salt catalyst, an oxidizing agent, an additive and alkali into a reactor, performing dissolving into an organic solvent, performing stirring to react at 50-70 DEG C, and separating and purifying the reaction product to obtain the polysubstituted benzodihydrofuro heterocyclic compound, the reaction formula of the preparation method is shown as a formula (I). According to the method, the alkyne ketoxime ether and the o-iodophenyl alkenyl ether which are simple and easy to obtain are used as reaction raw materials to synthesize a seriesof polysubstituted benzodihydrofuro heterocyclic compounds, and the method has the characteristics of simple and easy-to-obtain raw materials, convenience in operation, mild conditions, high step economy, wide substrate applicability, good functional group tolerance and the like.

The invention relates to a method for primary amine-directed construction of 6-(4-bromo-2-fluorophenyl)indolo[1,2-a]quinoxaline. In a reaction test tube, 2-(1H-indol-1-yl)benzenamine and 4-bromo-2-fluorobenzoyl formic acid are added and taken as raw materials, and an acylation/cyclization reaction is carried out to prepare the 6-(4-bromo-2-fluorophenyl)indolo[1,2-a]quinoxaline in a high yield mode. The method for the primary amine-directed construction of the 6-(4-bromo-2-fluorophenyl)indolo[1,2-a]quinoxaline has the advantages that primary amine is taken as a traceless directional base to increase the step economy of the reaction; the raw materials required for the reaction are cheap and easy to obtain, the conditions are mild, the operation is simple, the selectivity is single, the separation yield is high, the industrial production is facilitated, and the method meets the development needs of green organic chemistry.

The invention discloses a method for constructing 2-chloro-6-phenylindolo[1,2-a]quinoxaline by primary amine directing. 4-chloro-2-(1H-indole-1-yl)aniline and benzoyl formic acid are added into a reaction tube and used as raw materials, and high-yield 2-chloro-6-phenylindolo[1,2-a]quinoxaline is obtained by acylation/cyclization reaction. According to the method, primary amine is used as a traceless directing group, and thus the economical efficiency of the reaction steps is increased; and the raw materials required for the reaction are cheap and easy to obtain, conditions are mild, the operation is simple, the selectivity is single and the separation yield is high, therefore, the method facilitates industrial production and is in line with the development needs of green organic chemistry.

The invention discloses a polyfluoroalkenyl substituted oxazole compound and a preparation method thereof. The preparation method comprises the following steps: adding a reaction raw material formed by mixing an N-acyl enamine compound and a perfluoroalkyl iodide into an alkali accelerant and a solvent, stirring and reacting for 1-24 hours in an air atmosphere at room temperature, determining a reaction process by TLC detection, obtaining a reaction solution after the reaction is finished, finally, sequentially washing, extracting and drying the reaction solution, and carrying out column chromatography separation to obtain the polyfluoroalkenyl substituted oxazole compound. According to the preparation method, the required raw materials are simple and easy to obtain, various functional group tolerance and substrate ranges are achieved, and natural products and pharmaceutical active molecular skeletons can be introduced, the preparation method disclosed by the invention is mild in reaction condition, does not need an expensive transition metal catalyst, and meets the requirements of green and economic chemistry, and according to the preparation method, a five-membered oxazole heterocyclic ring does not need to be constructed and synthesized in advance, and the highest step economy is achieved.

The invention belongs to the technical field of organic synthesis, and discloses a halogenated oxaallylamine compound as well as a preparation method and application thereof. The preparation method comprises the following steps: adding copper halide into a reactor, then adding an organic solvent, conducting dissolving, conducting stirring and reacting at 35-45 DEG C, and separating and purifying the reaction product to obtain the halogenated oxaallylamine compound. The reaction formula of the preparation method is as shown in a formula (I). According to the method, allene ether and aromatic amine which are simple and easy to obtain are used as reaction raw materials to synthesize a series of halogenated oxaallylamine compounds, and the method has the characteristics of simple and easy-to-obtain raw materials, convenience in operation, mild conditions, high step economy, wide substrate applicability, good functional group tolerance and the like.