10 results about "Cyclononane" patented technology

The invention discloses a catalyst for preparing ultrahigh molecular weight polyoxyethylene as well as a preparation method and application thereof, and relates to the technical field of catalyst preparation. The preparation method of the catalyst comprises the following steps: S1, carrying out a reaction on 6-hexamethylenediamine and allyl acrylate to generate an intermediate 1, S2, carrying out a reaction on the intermediate 1 and diphenylphosphine to generate an intermediate 2, S3, carrying out a reaction on the intermediate 2 and allyl bromide to generate an intermediate 3, and S4, carrying out a reaction on the intermediate 3 and 9-boron bicyclo [3.3. 1] nonane. The prepared catalyst is high in catalytic activity, ultrahigh molecular weight polyoxyethylene can be prepared, and the molecular weight distribution of the prepared ultrahigh molecular weight polyoxyethylene is narrow.

The invention relates to a preparation method of (S, S)-2, 8-diazabicyclo [4, 3, 0] nonane and an intermediate of the (S, S)-2, 8-diazabicyclo [4, 3, 0] nonane. Specifically, the invention discloses a method for preparing (S, S)-2, 8-diazabicyclo [4, 3, 0] nonane from a cheap raw material 2-chloronicotinic acid through an esterification reaction, a substitution reaction, a reduction reaction and an asymmetric hydrogenation reaction, and the method is novel in route, simple to operate, high in product yield, good in purity, safe, environment-friendly and very suitable for industrial production.

The present invention is related to a compound of formula (I):whereinR1 is selected from the group consisting of hydrogen, methyl and cyclopropylmethyl;AA-COOH is an amino acid selected from the group consisting of 2-amino-2-adamantane carboxylic acid, cyclohexylglycine and 9-amino-bicyclo[3.3.1]nonane-9-carboxylic acid;R2 is selected from the group consisting of (C1-C6)alkyl, (C3-C8)cycloalkyl, (C3-C8)cycloalkylmethyl, halogen, nitro and trifluoromethyl;ALK is (C2-C5)alkylidene;R3, R4 and R5 are each and independently selected from the group consisting of hydrogen and (C1-C4)alkyl under the proviso that one of R3, R4 and R5 is of the following formula (II)whereinALK′ is (C2-C5)alkylidene;R6 is selected from the group consisting of hydrogen and (C1-C4)alkyl; andR7 is selected from the group consisting of H and an Effector moiety;or a pharmacologically acceptable salt, solvate or hydrate thereof.

This invention relates to a method for preparing 6-benzyl-1,2,3,4-tetrahydro-6H-pyrrolo[3,4-B]pyridine-5,7-dione and its application. The method for preparing 6-benzyl-1,2,3,4-tetrahydro-6H-pyrrolo[3,4-B]pyridine-5,7-dione involves reacting (1R,6S)-8-benzyl-7,9-dioxo-2,8-diazabicyclo[4,3,0]nonane in an organic solvent under blue light irradiation with the aid of a photosensitizer and an oxidizing agent to obtain 6-benzyl-1,2,3,4-tetrahydro-6H-pyrrolo[3,4-B]pyridine-5,7-dione. This preparation method not only has mild reaction conditions, short reaction time, simple operation, and environmental friendliness, but also has high product conversion rate and good selectivity. It can be used for large-scale industrial production and can be better applied to the synthesis of moxifloxacin, thereby improving the utilization rate of raw materials in the synthesis of moxifloxacin.

The present invention provides an industrial production method for a 9-iodine-9-borane bicyclo[3.3.1] solution, comprising the steps of: 1) passing an appropriate amount of dry hydrogen iodide gas generated on site into a mixture of a 9-borane bicyclo[3.3.1]nonane dimer and an organic solvent under inert gas protection at 15 to 25° C. to carry out a heterogeneous system reaction; 2) after stopping the introduction of hydrogen iodide, stirring for 1 to 20 hours at 15 to 25° C., degassing the mixture by vacuum pumping negative pressure for 5 to 10 minutes and replenishing nitrogen to obtain a colorless transparent solution, which is then appropriately diluted to obtain a commercially available 9-iodine-9-borane bicyclo[3.3.1]nonane solution. The present invention is suitable for the industrial production of a 9-iodine-9-borane bicyclo[3.3.1]nonane solution and has the advantages of mild reaction conditions, safe and simple operation, low environmental production cost, and a stable production process.

A combination of the present invention is an effective therapy for glaucoma, in particular a combination of 2-propanyl 4-{(3S,5aR,6R,7R,8aS)-6-[(1E,3R)-4-(2,5-difluorophenoxy)-3-hydroxy-1-buten-1-yl]-7-hydroxyoctahydro-2H-cyclopenta[b]oxepin-3-yl}butanoate and a β-blocker, is useful as an agent for treating glaucoma since the combination enhances intraocular pressure lowering action compared to a single administration of each drug and has an effect of maintaining intraocular pressure lowering action.

The present invention relates to a crystalline form of the compound (22R,24S,5S)-24,35-difluoro -5-methyl-4-oxa-7,9-diaza-1(5,3)-pyrazolo[1,5-a]pyrimidin-3(3,2)-pyridin-2(1,2) -pyrrolidincyclononuan-8-one of formula (I) and a preparation method therefor. The crystalline form provided in the present invention has favorable properties in terms of stability and hygroscopicity, and is suitable for drug research and industrial production. The crystalline form has significant value for the optimization and development of the drug in the future.

The invention discloses a green synthesis method of moxifloxacin hydrochloride, which comprises the following steps: under a heating condition, reacting moxifloxacin cyclization ester with moxifloxacin ((S, S)-2, 8-diazabicyclo [4, 3, 0] nonane) in a solvent, alkali and catalyst system to obtain moxifloxacin ester, and then carrying out hydrolysis one-pot method in an acidic system to obtain the moxifloxacin hydrochloride. The moxifloxacin hydrochloride is directly prepared. The invention provides a green synthesis method of moxifloxacin hydrochloride. According to the green synthesis method, moxifloxacin is obtained through direct reaction of moxixane cyclization ester and moxixane. According to the method, the moxifloxacin serving as a target product is synthesized by taking the moxixane cyclization ester as a raw material without forming a chelate compound with boric acid ester and directly reacting with the moxixane through a one-pot method, no three wastes are generated in the preparation process, and the method has the advantages of short reaction steps, mild conditions, high yield and the like.

The invention relates to a preparation method and application of 6-benzyl-1, 2, 3, 4-tetrahydro-6H-pyrrolo [3, 4-B] pyridine-5, 7-diketone, and the preparation method of the 6-benzyl-1, 2, 3, 4-tetrahydro-6H-pyrrolo [3, 4-B] pyridine-5, 7-diketone comprises the following steps: in an organic solvent, by taking (1R, 6S)-8-benzyl-7, 9-dioxo-2, 8-diazabicyclo [4, 3, 0] nonane as a raw material, under the action of a photosensitizer and an oxidizing agent, carrying out a reaction on (1R, 6S)-8-benzyl-7, 9-dioxo-2, 8-diazabicyclo [4, 3, 0] nonane and ( The preparation method comprises the following steps: taking 2, 2, 3, 4-tetrahydro-6H-pyrrolo [3, 4-B] pyridine-5, 7-diketone as a raw material, and reacting under the irradiation of a blue light source to obtain 6-benzyl-1, 2, 3, 4-tetrahydro-6H-pyrrolo [3, 4-B The preparation method is mild in reaction condition, short in reaction time, simple to operate, environment-friendly, high in product conversion rate and good in selectivity, can be used for industrial large-scale production and can be better applied to synthesis of moxifloxacin, and the utilization rate of raw materials in synthesis of moxifloxacin is increased.