43 results about "Salmeterol" patented technology

The present invention relates to an improved process for preparing 4-(6-bromohexyloxy)-butylbenzene by reacting 4-phenylbutanol with 1,6-dibromohexane in the presence of a base and a phase transfer catalyst, wherein 4-phenylbutanol in a diluent is metered into a mixture consisting of 1,6-dibromohexane, a base, a phase transfer catalyst and a diluent, and the use of the 4-(6-bromohexyloxy)-butylbenzene thus prepared for producing salmeterol in a method known per se.

The present invention relates to a pharmaceutical formulation for use in the administration of a long-acting β2-agonist by inhalation. In particular this invention relates to a chemically stable, highly efficient salmeterol HFA solution formulation to be administered by pressurized metered dose inhalers (pMDIs) characterized by a deep lung penetration. The invention also relates to methods for the preparation of said formulation and to its use in respiratory diseases such as asthma and chronic obstructive pulmonary disease (COPD).

The invention relates to the technical field of preparation and application of chiral high-performance liquid chromatography column materials, and discloses preparation and application of beta-CD-D2 high-performance liquid chromatography chiral column material. A high-performance liquid chromatography chiral column is prepared from beta-CD-D2 and is used for splitting chiral medicine enantiomers. The preparation and the application of the beta-CD-D2 high-performance liquid chromatography chiral column material comprise the following steps: 1, constructing a chiral environment by using beta-CD-D2, bonding the chiral environment with high-performance liquid chromatography silica beads into a fixed phase filler, then preparing the fixed phase filler into a chiral column, and applying the chiral column into high-performance liquid chromatography; 2, finding out an optional formula and an optional condition by using a proper characterization means, and optimizing the method and the condition; 3, establishing a preparation method of a salmeterol single enantiomer by using the prepared beta-CD-D2 chiral column, and splitting a chiral compound by using a cyclodextrins derivative for the first time; and 4, splitting drugs by using the prepared beta-CD-D2 chiral column, and establishing a method for splitting and qualitatively and quantitatively analyzing seven chiral drugs including salmeterol, terbutaline, procaterol, cetirizine, lamivudine, cefuroxime and ceftriaxone.

The invention discloses a method for preparing an anti-asthmatic medicament of salmeterol. The method comprises the following steps of: adding paraxylene, parahydroxyphenylacrylic acid, formaldehyde and acid medium into a reactor, heating, cooling, filtering, washing and drying to obtain 3-hydroxymethyl-4-hydroxyl-phenylacrylic acid; adding the 3-hydroxymethyl-4-hydroxyl-phenylacrylic acid into the reactor, then adding oxyful, lipase and ethyl acetate to finally obtain 3-hydroxymethyl-4-hydroxyl-(beta-hydroxy)-phenylpropyl aldehyde, adding the 3-hydroxymethyl-4-hydroxyl-(beta-hydroxy)-phenylpropyl aldehyde and 6-(4-phenylbutoxy)hexylamine into the reactor, heating for reflowing, cooling, filtering, adding sodium borohydride in batches into filtrate, stirring at normal temperature, then evaporating to dryness, extracting, combining organic layers, drying, filtering and evaporating to dryness to obtain a solid, and separating by using the column chromatography to obtain the final product. The invention has novel and short synthetic route, convenient experiment operation, higher yield of the target product and lower production cost.

The invention discloses a preparation method for salmeterol expressed by formula 3. The preparation method comprises the following steps: in a solvent, under the catalysis of palladium carbon, causing the compound 1, compound 2 and hydrogen to be subjected to reduction ammoniation reaction, thereby obtaining the salmeterol. The preparation method provided by the invention has the advantages of mild reaction conditions, simple post-processing, lower cost, higher yield and easiness in realization of industrialization.