12 results about "Aza Compounds" patented technology

The invention provides a boron-nitrogen heterocyclic compound as well as an intermediate and a preparation method thereof, the boron-nitrogen heterocyclic compound has a structure as shown in a general formula (1), and is prepared by taking compounds as shown in a formula A, a formula B and a formula C as intermediates. Compared with similar carbon skeleton molecules, the boron-nitrogen heterocyclic compound provided by the invention shows an excellent narrow-band luminescence property. The half-peak width of the emission spectrum of the boron-aza compound is as low as 6.4 nm, and meanwhile, the fluorescence quantum yield is as high as 97%.

The invention belongs to the technical field of phytochemistry, and particularly relates to a benzo [e] pyrrolo [1, 2-a] aza # imgabs0 # compound as well as a preparation method and application thereof. The preparation method comprises the following steps: fermenting cigar stem barks, drying the fermented cigar stem barks in the sun, crushing and sieving to obtain a material a; adding a first solvent into the material a for reflux extraction to obtain an extracting solution, concentrating the extracting solution, adding a second solvent for extraction, combining the extracted extraction phases, and performing vacuum concentration to obtain an extract b; carrying out silica gel column chromatography on the extract b, eluting with chloroform-acetone eluent, monitoring by TLC (Thin Layer Chromatography), and collecting the eluent; and purifying the eluent by using a sephadex column, and separating and purifying by using high performance liquid chromatography to obtain the benzo [e] pyrrolo [1, 2-a] aza # imgabs 1 # compound with tobacco black shank resisting activity. The compound is novel in structure, has relatively good black shank resistance activity, can be used as a lead compound for resisting tobacco black shank, and is used for research and development of biological pesticides for preventing and treating tobacco black shank.

A tetra-aza corand compound of formula (Ia) and compound of formula (Ib) and salts thereof. The tetra-aza corand of formula (Ia) and (Ib) of the present invention relates to novel corand entity having a substantially enclosed volume and a framework structure, the compounds are designed as therapeutic carriers for molecule therapeutics delivery and pharmaceutical compositions thereof.

The invention discloses a benzo-aza compound as well as a preparation method and application thereof. The benzazepine compound and the pharmaceutically acceptable salt of the benzazepine compound prepared by the invention have relatively high sensitivity and very strong cytotoxic activity to human colon cancer cells HCT116 tumor cells. The triethylene diamine catalyst is adopted in the process of preparing the benzo-aza compound, the reaction conditions are relatively conventional, the reaction process is mild, simple and convenient, the operation is easy, the cost is low, and the method is suitable for industrial large-scale production; according to the method, various substrates are used as reactants, products with various and complex structures are obtained, the yield is high, and the application range of the method is widened. The compound prepared by the preparation method disclosed by the invention has relatively high cytotoxic activity on human colon cancer cells HCT116. Therefore, the preparation method provided by the invention can provide a basis for screening the benzazepine compound with good activity on tumor cells, and is beneficial to further screening out compounds with more excellent biological activity.

The present invention discloses a near-infrared emitting amide-fused aza-BODIPY compound and its preparation method. The synthesis method is as follows: 5-aldehyde-2-thiopheneboronic acid and 1-bromo-1-aryl-2,2-diphenylethylene undergo a Suzuki reaction to obtain intermediate 1, which is then oxidized to obtain intermediate 2. This intermediate is further cyclized with diisopropyl succinate to obtain intermediate 3, which is then cyclized and complexed with 5-(pyridine-3-alkynyl)pyridine-2-amine to obtain a near-infrared emitting amide-fused aza-BODIPY compound. The amide-fused aza-BODIPY fluorescent dye prepared by the present invention has a Stokes shift of 72 nm and a maximum fluorescence emission peak of 755 nm.

The application relates to a chiral 1,4-benzoxazepine compound and preparation and application thereof, which has a structure as shown in formula 1: wherein R 1 is one of a phenyl group, a p-methylphenyl group and a p-methoxyphenyl group; R 2 , R 3 are each independently one of a methyl group and a methoxy group; and R 4 is one of a p-nitrobenzenesulfonyl group and a p-toluenesulfonyl group. Compared with the prior art, raw materials of the application are easy to prepare, the catalyst has low consumption, high catalytic efficiency, flexible stereoselectivity control, simple ligand modification, and the additional acid catalyst is equivalent.

The invention relates to 1,5-benzothiazepine and 1,2,5-benzothiadiazepine derivatives of formula (I). These compounds are bile acid modulators having apical sodium-dependent bile acid transporter (ASBT) and / or liver bile acid transport (LBAT) inhibitory activity. The invention also relates to pharmaceutical compositions comprising these compounds and to the use of these compounds in the treatment of cardiovascular diseases, fatty acid metabolism and glucose utilization disorders, gastrointestinal diseases and liver diseases.

The present application relates to the field of organic synthesis, and is a preparation method of imidazo six-membered nitrogen heterocyclic compounds containing isothiourea fragments for medicines and intermediates. The method uses nitrogen atom ortho isocyanomethyl-substituted pyridine, pyrimidine, pyrazine, quinoline and other nitrogen-containing heteroaromatic rings as raw materials, reacts with various disulfides under the action of N-chlorosuccinimide (NCS) and a catalytic amount of TEMPO, and intramolecularly cyclizes to form imidazo six-membered nitrogen heterocyclic compounds containing isothiourea fragments. The method can realize intramolecular ring closure in one step, form imidazo[1,5a] nitrogen-containing heteroaromatic rings containing isothiourea fragments, construct various imidazo[1,5a] nitrogen-containing heteroaromatic rings containing isothiourea fragments, has high yield, low raw material cost, can realize large-scale industrial production, and has market application prospect.

The invention belongs to the technical field of chemical medicine preparation, and particularly relates to a benzo [b] indeno [1, 2-e] [1, 4] diaza compound as well as a preparation method and application thereof. The structure of the compound is shown as a formula I. The preparation method comprises the following steps: by taking a compound shown as a formula II structure and a compound shown as a formula III structure as reaction substrates, adding an oxidizing agent and a solvent, and carrying out a heating reaction, thereby obtaining the compound. The preparation method provided by the invention is simple and convenient to operate, good in economical efficiency, environment-friendly and wide in substrate application range, and the compound has good application in preparation of medicines for preventing or treating cancers.

Compound of formula (l): wherein R1 represents a hydrogen atom or a heterocyclic, cyano, alkoxycarbonyl, alkylsulphoriylaminoalkyl or N-hydroxycarboximidamide group, process for its preparation and pharmaceutical composition containing it for use as a modulator of the AMPA (a-amino-3 hydroxy-5 -methyl-4-isoxazole-propionfc acid) receptor.

The present disclosure provides, in part, benzothia(dia)zepine compounds, and pharmaceutical compositions thereof, and methods of treating Hepatitis B virus (HBV) and Hepatitis D virus (HDV) infections.