Azlocillin

ChEBI: A semisynthetic penicillin antibiotic used in treating infections caused by Pseudomonas aeruginosa, Escherichia coli, and Haemophilus influenzae.

Step S1, under room temperature conditions, 30 parts of ampicillin trihydrate was added to the reaction vessel in parts by weight, 60 parts of acetone, 250 parts of water, Dioxane and tetrahydrofuran, 5 parts, Stir well;The ratio by weight of dioxane to tetrahydrofuran was 4: 1;Step S2, When the temperature of the material in the reaction vessel was reduced to 10 to 15 ° C, 9 parts of triethylamine was added dropwise, Stirring to completely clear the solution in the reaction vessel;In step S3, When the temperature of the material in the reaction vessel is reduced to 5 to 10 ° C, Slowly add1- chlorocarbonyl-2-imidazolidinone10.92 parts, Keep 15 , stirring reaction 3h;In Step S4, hydrochloric acid was added to the reaction vessel, Adjust the pH to 3 ~ 4, Placing at 3 ~ 5 ° C under the conditions of azlocillin acid crystallization, precipitate precipitation;Step S5, filtration, sedimentation, After rinsing with acetone and drying in vacuo, Obtain azlocillin acid.In step S1, the above-mentioned method is used to prepare In step S1, the method comprises the following steps of: preparing aloselenic acid in water for injection, the ratio of aloselic acid to water for injection is 1: 3.5, cooling to 5-8 ;Step S2, adding sodium hydroxide solution, adjust the pH to 7.0 ~ 7.6;Step S3, adding medicinal activated carbon, agitating for 20-30 minutes, filtering the medicinal active carbon with 0.8mum porous filter membrane, Step S4, the filtrate after removing the medicinal active carbon is sterilized and filtrated to obtain the sterile filtrate; the sterilizing filtration comprises filtering twice, filtering with 0.45mum microporous filter, filtering with 0.22mum microporous membrane filter.In step S5, the sterile filtrate is freeze-dried to obtain freeze-dried powder of Step S1, under room temperature conditions, 30 parts of ampicillin trihydrate was added to the reaction vessel in parts by weight, 60 parts of acetone, 250 parts of water, Dioxane and tetrahydrofuran, 5 parts, Stir well;The ratio by weight of dioxane to tetrahydrofuran was 4: 1;Step S2, When the temperature of the material in the reaction vessel was reduced to 10 to 15 C, 9 parts of triethylamine was added dropwise, Stirring to completely clear the solution in the reaction vessel;In step S3, When the temperature of the material in the reaction vessel is reduced to 5 to 10 C, Slowly add1- chlorocarbonyl-2-imidazolidinone10.92 parts, Keep 15 , stirring reaction 3h;In Step S4, hydrochloric acid was added to the reaction vessel, Adjust the pH to 3 ~ 4, Placing at 3 ~ 5 C under the conditions of In step S1, 25 parts of ampicillin trihydrate, 55 parts of acetone, 240 parts of water, 4 parts of dioxane and tetrahydrofuran were added in the reaction container in the reaction container under the condition of room temperature, and the mixture was stirred well; dioxane and tetrahydrofuran Of 3: 1 by weight;Step S2, when the temperature of the material in the reaction vessel is reduced to 10-15 DEG C, 6 parts of triethylamine is added dropwise, and the solution in the reaction vessel is completely clarified by stirring;In step S3, when the temperature of the material in the reaction vessel is reduced to 5 to 10 DEG C, 9.10 parts of 1-chloroformyl-2-imidazolidinone is slowly added and kept at 5 to 10 DEG C for 2.5 hours.Step S4: adding hydrochloric acid to the reaction vessel, adjusting the pH to 3-4 and carrying out crystallization of aloselenic acid under the condition of 3 to 5 DEG C to precipitate the precipitate;In step S5, the precipitate was filtered off, washed with acetone and dried in vacuo to obtain

It is a semi-synthetic broad-spectrum antimycin and has antibacterial activity against Pseudomonas aeruginosa, anaerobic bacteria, Escherichia coli, etc.