33 results about "Terbutaline sulphate" patented technology

The invention provides a method for preparing terbutaline sulphate B crystal form. The method comprises: selecting a solvent, dissolving 1-(3,5-dibenzyloxy phenyl)-2-n-tert-butyl aminoethanol into the solvent, removing benzyl groups through hydrogenolysis by a general method, obtaining terbutaline free alkali, and adding sulfuric acid into the terbutaline free alkali to form terbutaline sulphate of crystal form B; or dissolving terbutaline sulphate of non-crystal form B into the solvent, stirring the terbutaline sulphate of the non-crystal form B in the solvent at a certain temperature until the terbutaline sulphate of the non-crystal form B is converted into the terbutaline sulphate B crystal form through dissolution and lixiviation, and reclaiming the leached terbutaline sulphate B crystal form. The method has the advantage of obtaining the terbutaline sulphate B crystal form which has stable chemical and physical properties and meets the requirements of medical preparation.

The invention relates to a preparation method of terbutaline sulphate. The technical problems that according to an existing preparation method of terbutaline sulphate, high-pressure hydrogenation and other high-risk operations, and lithium methide, azomethane and other high-risk reagents exist, and cost is high are solved through the preparation method. 3,5-resacetophenone serves as a raw material, and terbutaline sulphate is obtained through hydroxyl protection, the bromination reaction, carbonyl reduction, the condensation reaction and sulphating. The preparation method can be suitable for industrially-produced terbutaline sulphate.

The invention discloses a preparation method of terbutaline derivatives, belongs to the field of compound preparation, and provides a synthesis method of a novel drug molecule acotiamide derivative, which is reasonable in process design, high in yield and convenient and controllable in operation process. The invention provides a preparation method of three terbutaline derivatives. The preparationmethod provided by the invention has the advantages of reasonable process design, strong operability, mild reaction conditions and high yield, and can realize industrial production. The series of terbutaline derivatives prepared by the method provide important basis for scientific evaluation of quality, safety and efficiency of the series of terbutaline derivatives, and have important applicationvalue.

The invention discloses a terbutaline derivative D and a synthesis method thereof, the structure of the terbutaline derivative D is as shown in a structural formula (I), and the specific synthesis route is as follows: 3, 5-dimethoxyphenylacetic acid and tert-butylamine are taken as raw materials, and the terbutaline derivative D is obtained through condensation, reduction, deprotection and substitution reaction. The terbutaline derivative D disclosed by the invention is simple in synthesis method, an intermediate generated in the synthesis process can be used as a terbutaline impurity, and a final product can be used as a bambuterol impurity for quality research.

The invention relates to a preparation method of terbutaline sulfate, which comprises the following steps: dissolving a compound of formula I or formula II into a solvent A, adding a metal catalyst for catalytic hydrogenation, so as to obtain 5-[2-[(1,1-dimethylethyl)amido]-1-ethoxyl]-1,3-resorcinol; after the reaction is finished, filtering, collecting filter liquor, adding a certain amount of concentrated sulfuric acid in the filter liquor, after stirring is stopped, recycling the solvent A, adding a solvent B into a residue, stirring to separate out a white crystal substance, performing suction filtration, thus obtaining the terbutaline sulfate. According to the method provided by the invention, the treating difficulty after the reaction is greatly reduced, the introduction of water and inorganic salt is avoided, and the product content is high; furthermore, the stability of the terbutaline sulfate is obviously improved by distilling the product under acidic conditions, the catalyst and the reaction solvents are recyclable, so that the environmental protection pressure is greatly reduced.

The invention provides a method for preparing terbutaline sulphate B crystal form. The method comprises: selecting a solvent, dissolving 1-(3,5-dibenzyloxy phenyl)-2-n-tert-butyl aminoethanol into the solvent, removing benzyl groups through hydrogenolysis by a general method, obtaining terbutaline free alkali, and adding sulfuric acid into the terbutaline free alkali to form terbutaline sulphate of crystal form B; or dissolving terbutaline sulphate of non-crystal form B into the solvent, stirring the terbutaline sulphate of the non-crystal form B in the solvent at a certain temperature until the terbutaline sulphate of the non-crystal form B is converted into the terbutaline sulphate B crystal form through dissolution and lixiviation, and reclaiming the leached terbutaline sulphate B crystal form. The method has the advantage of obtaining the terbutaline sulphate B crystal form which has stable chemical and physical properties and meets the requirements of medical preparation.

The invention discloses a synthetic method of terbutaline, which is characterized in that it comprises the following steps: (1) reacting 3,5-dimethoxyacetophenone with tetrabutylammonium tribromide to obtain 2- Bromo-1-(3,5-dimethoxyphenyl)ethanone; (2) react it with a reducing agent in methanol to give 2-bromo-1-(3,5-dimethoxyphenyl ) ethanol; (3) it is carried out ring-forming reaction under alkaline condition, generates 2-(3,5-dimethyloxyl) oxirane; (4) it is reacted with tert-butylamine, generates 1-( 3,5-dimethoxyphenyl)-2-tert-butylamino-ethanol; (5) demethylating it under acidic conditions to give 1-(3,5-dihydroxyphenyl)-2-tert-butyl The salt of amino-ethanol is terbutaline. In the present invention, the total molar yield is about 60%, which is much higher than that of the prior art, and is suitable for industrialized production.

The invention belongs to the field of pharmacy, and in particular relates to a preparation method of terbutaline. The technical points are as follows: a method for preparing terbutaline, S1. Add compound I and methylene chloride into the reaction kettle, stir and dissolve and then add acid anhydride; S2. After the reaction is completed, add dilute alkaline water into the system to fully stir and wash , collect the dichloromethane phase, and distill under reduced pressure to obtain a yellow oily substance, which is compound II; S3. add compound II, ethyl acetate, tert-butylamine, sodium hydroxide and oxidation protection agent to the reaction kettle; S4. step S3 completes the reaction Then add purified water to the system to wash the reaction solution in step S3, collect the ethyl acetate phase, and distill the ethyl acetate phase under reduced pressure to obtain terbutaline. The technical solution provided by the invention reduces the difficulty of post-reaction treatment, makes the intermediate compound easy to separate from the reaction system, avoids the occurrence of side reactions such as epoxy bond hydrolysis, and increases the stability and stability of the final product terbutaline. yield.

The invention belongs to the technical field of medicine, and particularly relates to a process treatment method for improving the stability of a terbutaline sulphate solution for nebulization. According to the invention, a metal chelating agent is adopted to passivate production equipment of a production line of the terbutaline sulphate solution for nebulization, and the passivated production equipment is employed to prepare liquid medicine. According to the process treatment method, metal ions on the surface of the production equipment are effectively removed through passivation of the equipment of the production line, and the stability of a product is guaranteed; and meanwhile, through an optimized packaging material, it is synchronously guaranteed that a final packaging material does not affect the product, nitrogen charging protection is not needed in the production process, a requirement on a production line is low, and production cost is saved.