476 results about "Azithromycin" patented technology

A novel, non-hygroscopic form of azithromycin is disclosed, as well as a method for preparing it by the gradual crystallization of azithromycin from ethanol by the addition of a minimal amount of water to effect crystal formation. Pharmaceutical compositions containing this novel form of azithromycin are also disclosed.

The present invention relates to the technical fields of organic chemistry and pharmaceutical chemistry, concretely discloses a synthetic method for a known compound tylosin. The synthetic method comprises the following steps: taking Azithromycin A as a raw material, the protected Azithromycin A can be obtained by Cbz-Cl and then oxidized through a modified Pfitznor-Moffat method, the protected ketone by Cbz can be obtained, ketone is reacted through Wittig-Horner, keto is conversed into alkenyl to obtain the protected alkene, the protected alkene is oxidized to obtain an epoxy compound protected by Cbz, the epoxy compound protected by Cbz is deprotected to obtain a deprotected epoxy compound under the catalysis of Pd / C, the deprotected epoxy compound is reacted with n-propylamine and is performed a ring-opening to obtain a tylosin crude product, the tylosin crude product and acid are carried out a salt forming and purifying, then tylosin can be obtained by resolving. The synthetic route is changed by the method of the invention, the super low-temperature is not employed in the route, and the tylosin enables the effective industrialization production.

The invention provides a tulathromycin intermediate, a preparation method of the tulathromycin intermediate, and a preparation method of the tulathromycin. The preparation method of the tulathromycin has the advantages of mild condition, convenience for operation, and low cost. The preparation method of the tulathromycin comprises the following steps of: using azithromycin A as a raw material; protecting 2'-hydroxy and 6'-amino in the azithromycin A through di-tert-butyl dicarbonate so as to obtain double-protective azithromycin A; carrying out Swern oxidation to 4''-hydroxy to the double-protective azithromycin A; salifying along with trifluoroacetic acid; and synchronously removing boc t-butyloxycarbonyl to obtain the azithromycin A bitrifluoroacetic acid salt of 4''-carbonyl; and then reacting with trimethylsulfonium bromide to obtain 4''-epoxy compound; and finally carrying out nucleophilic addition on the 4''-epoxy compound by n-propylamine so as to obtain the phosphate of tulathromycin; and further neutralizing via alkaline to obtain the target compound tulathromycin; and synchronously obtaining the tulathromycin intermediate of azithromycin A bitrifluoroacetic acid salt of 4''-carbonyl.

The invention discloses a method for preparing azithromycin. The method comprises the following steps of: in acid aqueous solution and under an action of potassium borohydride, performing the reduction reaction of erythromycinA6, 9-imine ether represented by a formula II, then performing methylation reaction, and putting the reaction products in a mixed solvent of water and halogenated hydrocarbons for hydrolysis reaction so as to obtain the azithromycin represented by a formula I. In the method, the reducer is properly consumed, the yield is high, and the cost of the preparation of the azithromycin is obviously reduced. The invention also relates to a method for preparing the erythromycinA6, 9-imine ether and erythromycinA9-oxime.

The invention provides a sterilizing method of a spherical phaeocystis culture solution, and relates to a microalgae culture solution. The method comprises the following steps: centrifuging algae solution which grows to an exponential phase, and removing supernatant; carrying out gravity suspension on algae cells with an f / 2 culture medium, centrifuging, and removing supernatant, repeating twice, and carrying out gravity suspension on the algae cells with the f / 2 culture medium; adding SDS (sodium dodecyl sulfate) and antibiotics, wherein the antibiotics are clindamycin, azithromycin, gentamicin, kanamycin, streptomycin, cefotaxime, ampicillin and rifamycin; culturing under illumination, centrifuging the algae solution and removing supernatant during culturing, carrying out gravity suspension on the algae cells with the f / 2 culture medium, centrifuging and removing supernatant, removing residual SDS and the antibiotics, transferring into the f / 2 culture medium, and culturing under illumination; and selecting survival transferred algae solution which is treated with SDS and the antibiotics, and detecting whether bacteria exist or not after the transferred algae solution grows to the exponential phase. The method is convenient to operate, complex operations, such as bacterium separation and test on sensitivity to antibiotics and the like, are avoided, and long-term treatment of high-concentration antibiotics has good sterilization effect.

The present invention relates to a method for treating non-infectious, inflammatory chronic posterior blepharitis in a subject. The present invention also relates to a method for treating chronic posterior blepharitis in a subject for over two weeks. The method comprises identifying a subject in need thereof, and topically administering to the eye of the subject a pharmaceutical formulation consisting essentially of an effective amount azithromycin. The present invention further relates to a method for treating dry eye secondary to blepharitis in a subject. The method comprises the steps of: identifying a subject suffering from dry eye secondary to posterior blepharitis, and topically administering to the eye of the subject a pharmaceutical formulation comprising an effective amount of azithromycin. The present invention further relates to method for reducing contact lens intolerance of a subject due to blepharitis or dry eye secondary to blepharitis.

The invention relates to a preparation method for a tulathromycin intermediate. The preparation method comprises the following steps: oxidizing 4'-hydroxyl of demethylazithromycin of which the hydroxyl is protected by acetyl under a mild condition to obtain ketone by using a dimethyl sulfoxide and acetic anhydride system, and continuing to epoxidize the obtained ketone to obtain an epoxide by using a phase transfer catalyst, wherein the intermediate epoxide of tulathromycin can be introduced into propylamine through an open loop, and is subjected to deprotection to obtain the tulathromycin. According to the reaction method, a phase transfer catalyst system is adopted for the first time in an exoxidizing process, reaction conditions are mild, and the method is high in yield and more suitable for industrial production.