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A kind of solid-phase synthesis method of ceftazidime hydrochloride
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A solid-phase synthesis method, the technology of ceftazidime, applied in the direction of organic chemistry, organic chemistry, etc., can solve the problems of low total yield, cumbersome operation, poor purity, etc.
Active Publication Date: 2019-02-01
SHANGHAI NEW ASIA PHARMA
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Problems solved by technology
[0008] The present invention aims to overcome the above-mentioned defects, aiming at the technical problems of low total yield, poor purity and cumbersome operation during the preparation of ceftazidime hydrochloride, it provides a preparation method and convenient post-treatment, simple operation, and Method for solid-phase synthesis of ceftazidime hydrochloride with high yield and purity not lower than 99.5%
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Embodiment
[0082] Embodiment one: embodiment one: the bridging of 7-APCA and solid phase carrier
[0083]
[0084] In the glazed glass column, 30g 7-APCA is reacted with chloromethyl resin in 100ml DMF, and TLC detects that there is no raw material residue, so that it is fully bridged with the solid phase carrier, and after the reaction is completed, use N2 (argon, air, Gases such as helium) flow to remove solvent, then wash the resin successively with 100ml of dichloromethane and pyridine (or solvents such as chloroform, toluene) respectively, and directly carry out the next step reaction.
[0085] In Embodiment 1, the chloromethyl resin can also be replaced by polystyrene-styrene divinyl cross-linked resin, polyacrylamide, polyethylene-glycol resin, carboxyl resin, amino resin, hydrazide resin, and the like.
[0086] According to the functional group difference of the resin, the dosage ratio of 7-APCA and resin was adjusted. For example: when polystyrene and polyethylene resins are...
Embodiment 2
[0089] Embodiment two: prepare the ceftazidime tert-butyl ester of solid-phase bridge
[0090]
[0091] A. Add 60g of trimethylalkylacetamide and 200ml of dichloromethane solution into the glazed glass column, cool down to -20°C, and add 78g of 4-bromoacetylacetyl bromide under stirring. After the addition was completed, the reaction was incubated at -10°C for 4 hours, and after the reaction was completed, N 2 (Gas such as argon, air, helium) flow to remove solvent, solvent recovery can be reused, then wash the resin successively with 100ml of dichloromethane and pyridine (or solvents such as chloroform, toluene), and directly carry out the next step reaction.
[0092] In this step, 4-bromoacetylacetyl bromide can also be replaced by e.g.:
[0096] The amount of the amidating agent (such as: 4-bromoacetylacetyl bromide) is: the molar rati...
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Abstract
The present invention provides a solid phase synthesis method of ceftazidime hydrochloride, and the solid phase synthesis method is characterized in that: a raw material A is bridged on a solid support, and the solid support is removed after amidation, nitrosation, condensation cyclization reaction and etherification to obtain the ceftazidime hydrochlorid; according to the solid phase synthesis method for preparation of the ceftazidime hydrochloride, a postprocessing process after the reaction can be omitted, reaction procedures are greatly simplified, product loss in the postprocessing process can be reduced, the total yield is increased to more than 60%, the purity is increased to more than 99.5%, and production efficiency is improved.
Description
technical field [0001] The invention belongs to the field of chemical pharmacy, in particular to a solid-phase synthesis method of ceftazidime hydrochloride. Background technique [0002] Ceftazidime is a third-generation cephalosporin antibiotic created by GlaxoSmithKline. It is used for sepsis, lower respiratory tract infection, abdominal cavity and biliary tract infection, complicated urinary tract infection and severe skin and soft tissue infection caused by sensitive gram-negative bacilli. It is especially suitable for infection of immunocompromised persons caused by multiple drug-resistant Gram-negative bacilli, nosocomial infections, and central nervous system infections caused by Gram-negative bacilli or Pseudomonas aeruginosa. [0003] Ceftazidime hydrochloride is an important raw material for preparing ceftazidime, and its chemical name is [0004] (6R,7R)-7-[[(2Z)-2-(2-Amino-1,3-thiazol-4-yl)-2-(1-carboxy-1-methylethoxy)iminoacetyl ]amino]-8-oxo-3-(pyridin-1-iu...
Claims
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