33 results about "Dihydrobenzopyrans" patented technology

A process of making racemic [2S*[R*[R*[R*]]]] and [2R*[S*[S*[S*]]]]-(±)α,α′-[iminobis(methylene)]bis[6-fluoro-3,4-dihydro-2H-1-benzopyran-2-methanol] of the compound of the formula (I)and its pure [2S*[R*[R*[R*]]]]- and [2R*[S*[S*[S*]]]]-enantiomer compounds and pharmaceutically acceptable salts thereof.

Insecticidal (dihalopropenyl) phenylalkyl substituted dihydrobenzofuran and dihydrobenzopyran derivatives of Formula I are disclosed. These compounds provide unexpected insecticidal activity across a spectrum of insect pests combined with desirable physical properties including improved photostability. wherein x and y are integers independently selected from 0 or 1; and B is a bridging group*—(CR16R17)q—(CR18R19)r—(CR20R21)s—Lt—(CR22R23)u—(CR24R25)v—(CR26R27)w—,where the asterisk denotes attachment at A; and q, r, s, u, v and w are integers independently selected from 0, 1 and 2; and t is an integer selected from 0 and 1. A, D, E, G, M, R through R11, and R16 through R27, inclusively, are fully described herein. In addition, compositions comprising an insecticidally effective amount of at least one compound of formula I and methods of controlling insects by applying said compositions to a locus where insects are present or are expected to be present are also disclosed.

A medicinal composition for the prophylaxis and treatment of cachexia which comprises a compound of the formula:wherein R represents a hydrocarbon group that may be substituted or a heterocyclic group that may be substituted; Y represents a group of the formula -CO-, -CH(OH)-, or -NR3- (R3 represents an alkyl group that may be substituted); m is 0 or 1; n is 0, 1 or 2; X represents CH or N; A represents a bond or a bivalent aliphatic hydrocarbon group having 1 to 7 carbon atoms; Q represents oxygen or sulfur; R1 represents hydrogen or an alkyl group; ring E may have further 1 to 4 substituents, which may form a ring in combination with R1; L and M respectively represent hydrogen or may be combined with each other to form a bond, provided that when m and n are 0, X represents CH, A represents a bond, Q represents sulfur, R1, L and M respectively represent hydrogen, and ring E does not have further substituents, R does not represent dihydrobenzopyranyl; or a salt thereof.

Novel phenazine derivatives of formula (I)are disclosed. In particular, substituted 2,3-dihydro-1H-benzo[a]pyrano[2,3-c]phenazines are disclosed. The compounds can be used as anti-angiogenic and / or anti-tumor agents.

The invention relates to a solid-phase synthesis method of coumarin and an analogue (I) thereof and belongs to the field of organic chemistry. The method comprises the following steps: 1) taking 1% of cross-linked polystyrene resin as a carrier to prepare a polystyrene-supported seleno-succimide reagent (III); 2) using the III to induce phenyl acrylate (V) to perform intramolecular cyclization under the catalysis of trimethylsilyl trifluoromethanesulfonate so as to form 3-polystyrene-supported seleno-3,4-dihydro-benzopyran-2-ketone (VI); and 3) performing oxidation elimination on the VI via an oxidant so as to directly get the coumarin (I) without further separation. When the phenyl acrylate (V) is replaced by N-phenyl acrylamide, the analogue of the coumarin, namely a 2-quinolone compound, can be prepared through the same steps. The solid-phase synthesis method disclosed by the invention has the advantages of easily available raw materials, good product yield, high purity, simplicity and convenience in operation, simple post-treatment and great industrial application prospects.

This invention is attributed to the field of organic chemistry and specifically relates to the method to synthesize drug intermediates (R)-2-amino-1-((R)-6-fluoro-3, 4-dihydrochromeno) ethanol and (R)-2-amino-1-((S)-6-fluoro-3, 4-dihydrochromeno) ethanol. The method is that, drug intermediates (2R)-2-[(1R)-4, 4-dimethyl-3, 5-dioxocyclopentyl]-6-fluoro-4-chromanone and (2S)-2-[(1R)-4, 4-dimethyl-3, 5-dioxocyclopentyl]-6-fluoro-4-chromanone are adopted as raw materials and reduced by Clemmensens method with the products reacting with p-toluenesulfonyl chloride in pyridine. The consequent products are dissolved in solvent and dry ammonia is introduced for heating reflux. The total yield can be as much as 32%.

The invention discloses a preparation method of nebivolol used for preparing medicines for treating hypertension of slight or medium degrees, and an intermediate compound. The preparation method comprises the following steps: taking 6-fluoro-2-(1-hydroxy-2-paratoluensulfonyl oxygroup-ethyl)-3,4-dihydrobenzopyrans as an initial raw material, introducing amino, then coupling with 6- fluoro-3,4-dihydro-2-epoxy ethyl-2H-1-benzopyran, and preparing (S,R,R,R) and (R,S,S,S)-nebivolol. Compared with a prior art, the preparation method has the advantages of novel design, simple operation and high yield, the usage of hazardous reagent such as ssodium azide and sodium hydride can be avoided, a column chromatography purifying method is avoided, so that the preparation method conforms to industrial production.

The invention discloses a compound, namely (2R, 3R)-((2-(3,4-dihydroxyphenyl)-5,7-dihydroxyl-4-oxo-2,3-dihydrobenzopyran-3-yl) methylamino) methyl-2-phenylpropionate. The invention also discloses a preparation method for the compound and the application of the compound as a feed additive. When serving as the feed additive, the compound can specifically promote the growth of intestinal mucosa villus of livestocks, promote the growth of intestinal linings, reduce the intestinal tension and inhibit abnormal peristalsis, can reduce the feed discharging speed of intestinal tracts of the livestocks so as to enhance the digestive absorption of the intestinal tracts to nutritional components, and can obviously increase the daily weight increasing of the livestocks. The reduction of the intestinal tension contributes to water absorption in the intestinal tracts, and plays an obvious role of convergence and reducing functional diarrhea. The compound provided by the invention also has an effect of repairing intestinal mucosa, and can also obviously improve the immunity function of intestinal mucosa and disease resistance of the livestocks.

The invention discloses N-acylpyrazole derritol with a chemical formula represented by the formula I. In the formula, R is selected from C1-C2 alkyl, C3-C4 straight-chain or branched-chain alkyl, and C6H5; X(CH2)n, X=OH, NH2, NHAc, Cl, Br, or C6H5; and n=1, 2, 3 or 4. The preparation method of N-acylpyrazole derritol comprises steps that: (2R)-5-[7,8-dimethoxy-3,3a,4,9b-tetrahydrobenzopyrano[3,4-c]pyrazole-1-group]-2-(propylene-2-group)-2,3-dihydrobenzopyran-4-phenol and acyl chloride or anhydride are subject to a reaction according to a molar ratio of 1:1, such that N-acylpyrazole derritol is obtained. The invention also provides an application of N-acylpyrazole derritol in the preparations of neuraminidase inhibitors.

This invention relates to a synthetic method for beta1-receptor blocking agent and 2, 2'-[imino di(methylene)]-di-(6-fluorine-3, 4-dihydro-2H-1-benzopyrane-2-methanol) methanesulfonate. First, prepare 6-fluorine-3, 4-dihydro-1-[amino (methylene)]-2H-1-benzopyrane-2-methanol using 6-fluorine-3, 4-dihydro-2- oxirane group -2H-1- benzopyrane as raw material; then, use LiAlH4 to dispose and get the compound Li-Al amidate; finally, enable Li-Al amide to react with 6-fluorine-3, 4-dihydro-2-oxirane group-2H-1- benzopyrane to get NBL. Advantages:low cost, simple operation and high purity of NBL methanesulfonate.

The invention relates to a method for synthesizing 6-fluoro-3,4-dihydro-2H-1-benzopyran-2-carboxylic acid and alkyl ester thereof. 2,4-dibromoalkylbutyrate is used as a raw material, and the products are obtained by three-step reaction. According to the synthesizing method, the 6-fluoro-3,4-dihydro-2H-1-benzopyran-2-carboxylic acid and the alkyl ester thereof serving as target products are obtained without hydrogenation reduction of expensive Pd / C catalyst; and the reaction process is simple, the conditions are mild, the raw materials are easily obtained, and the yield is high.

The present invention provides a method for preparing a 2,3-dihydrobenzopyran-4-one derivative, and the method comprises the following steps: under nitrogen atmosphere at room temperature, dissolvinga 2-allyloxybenzaldehyde derivative represented by formula (I) and a benzoin derivative represented by formula (II) in an organic solvent, adding a photosensitizer, evenly mixing, placing under an ultraviolet lamp for light irradiation reaction, removing the solvent by rotary evaporation, and separating and purifying by silica gel column chromatography to obtain the resulting product 2,3-dihydrobenzopyran-4-one derivative. The preparation method solves the problems of cumbersome steps, low yield and poor environmental protection property of the existing synthesis method, can react under normaltemperature and normal pressure, and has the advantages of mild reaction conditions, no need of transition metal catalysis, simple operation, no pollution, safety, environmental protection, low costand the like. R1 and R2 are hydrogen, halogen or alkyl.

The invention belongs to the technical field of medicine and discloses a medicine for reducing blood pressure. The molecular formula of the medicine for reducing blood pressure is 9-octyl-9,10-dihydrobenzopyran [8,7-e][1,3]oxazine-2(8H)-ketone(LYF-5). The LYF-5 has endothelium and non-endothelium dependent vasodilatation effect; the mechanism and the endothelium dependent NO-cGMP signal pathway and the non-endothelium dependent signal pathway mainly inhibit external calcium from flowing inside and inhibit calcium on a sarcoplasmic reticulum from releasing through a VDCC; and the result of theinvention provides a clue for developing the LYF-5 into a new medicine for reducing blood pressure.

The invention relates to the new synthesized compound i.e. dihydrobenzo pyrone type and the application thereof, and belongs to the field of the chemical drug. The experiment results shows that the compound (I) can kill the breast cancer cell MCF7 expressing ER Alpha 66, FR Alpha 46 and ER Alpha 36. Moreover, the compound (I) can be served as the regulator of the estrogen receptor ER Alpha 36 fortreatment of the illness caused by the unusual expression of the estrogen receptor ER Alpha 36, such as the tumor, the osteoporosis, the asthma, the heart disease and the senile dementia, etc.