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Prednisolone synthesis -
Recent advances in the design and synthesis of prednisolone and methylprednisolone conjugates.
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❾-50%}Synthesis of prednisolone from steroids extracted from Agave sisalana Perr.
Therefore, new drug delivery systems are being developed, with the aim of improving the physicochemical properties of glucocorticoids while avoiding undesirable side effects associated with systemic administration.
Here we discuss the design and synthesis of conjugates of prednisolone PD , methylprednisolone MPD and similar glucocorticoids. In this review, possibilities for targeting inflammatory sites, and reducing dosages and administration frequency through increasing drug circulation time are discussed.
In 3 and 20 deprotection reactions of critical process, conventional fabrication techniques be prior to The system of sodium nitrite solution and hydrochloric acid solution carries out reaction and obtains nitrous compound, then carries out resin hydrolyzing and be further purified removal Prednisolone is obtained after impurity.
Why the deprotection reaction mode combined using nitrosation and resin hydrolyzing, is due to strong It is stronger to the destruction of steroidal ring structure under acid condition, need by adding the reactive mode removal nitrosation of resin hydrolyzing anti- Should during a large amount of impurity for producing and improve product appearance. But still need in deprotection reaction To carry out under strong acid system, it is impossible to avoid destruction and solution loss to steroidal ring structure under strong acidic condition.
Prednisolone adopts pyridine as solvent and the catalyst of reaction with the traditional handicraft of acetic anhydride esterification. Chinese patent So can not only produce substantial amounts of Industrial wastewater, and cannot can bring the solution loss of product with avoiding.
Due to the stable chemical nature of DMF and DMSO, it is difficult to Degraded with conventional biological processes, it is necessary to waste water is processed using expensive membrane separation technique, quantity of wastewater effluent is still suffered from excessive, industrial The deficiencies such as cost for wastewater treatment height.
The present invention is directed to the deficiencies in the prior art, there is provided a kind of preparation technology of prednisolone acetate. What the present invention was provided Method significantly reduces the consumption of liquid supplementary material in reaction system, and product yield is high, and amount of industrial wastewater is greatly decreased, and effectively drops Low cost of material and environmentally friendly cost, are adapted to industrial scale production.
It is not required to increase solvent in addition using present invention process, not only significantly carries The high batch production capacity of reactor, and generation is avoided because solvent is using bringing a large amount of reluctant industrial wastewaters, keep away The strip loss of solvent in last handling process is exempted from. Present invention process has technical process simple, is conducive to environmental conservation, cost Advantage that is low, being suitable for industrialized great production.
Mark Item. Current Pharmaceutical Design. Close Print this page. Content: Citation Only. Citation and Abstract. Close About this journal. Related Journals Current Probiotics. Current Medicinal Chemistry. Current Topics in Medicinal Chemistry. Current Respiratory Medicine Reviews. Anti-Infective Agents. Infectious Disorders - Drug Targets. Current Molecular Pharmacology.
Glucocorticoid drugs are commonly used in the treatment of many acute and chronic inflammatory diseases. However, application of these steroids is limited because of their physico-chemical properties, such as very low water solubility.
Glucocorticoids also exhibit serious adverse side effects. Therefore, new drug delivery systems are being developed, with the aim of improving the physicochemical properties of glucocorticoids while avoiding undesirable side effects associated with systemic administration. Here we discuss the design and synthesis of conjugates of prednisolone PDmethylprednisolone MPD and similar glucocorticoids. In this review, possibilities for targeting inflammatory sites, and reducing dosages and administration frequency through increasing drug circulation time are discussed.
This review summarises synthetic approaches for the preparation of covalent conjugates, which are divided into two groups: low molecular weight conjugates and polymeric conjugates.
These two groups are further divided into subgroups based on the chemical structure of the conjugates. Published results from in vitro and in vivo testing of prepared conjugates are also discussed. Abstract Glucocorticoid drugs are commonly used in the treatment of many acute and chronic inflammatory diseases.
Publication types Review.
Scheme 8 shows the step synthesis of prednisolonecarboxylate ester (48) from hydrocortisone (1). The OH and OH groups of hydrocortisone were. Here we discuss the design and synthesis of conjugates of prednisolone (PD), methylprednisolone (MPD) and similar glucocorticoids. In this review, possibilities. Effect of prednisolone on prostaglandin synthesis by rectal mucosa in ulcerative colitis: investigation by laminar flow bioassay and radioimmunoassay. Prednisolone acetate is The important intermediate of synthesis prednisolone and other steroid drugss, in steroid drugss field using extremely wide. Glucocorticoid drugs are commonly used in the treatment of many acute and chronic inflammatory diseases. However, application of these steroids is limited. Login to Download Close. Why the deprotection reaction mode combined using nitrosation and resin hydrolyzing, is due to strong It is stronger to the destruction of steroidal ring structure under acid condition, need by adding the reactive mode removal nitrosation of resin hydrolyzing anti- Should during a large amount of impurity for producing and improve product appearance. The process is simple in process, beneficial to environmental protection, low in cost and suitable for industrial large-scale production. Meta-Inflammation and Obesity. But still need in deprotection reaction To carry out under strong acid system, it is impossible to avoid destruction and solution loss to steroidal ring structure under strong acidic condition.Application publication date : The invention relates to a preparation process of prednisolone acetate. The preparation process comprises the steps that under the action of 4-dimethylamino-pyridine, no solvent needs to be additionally added, prednisolone and acetic anhydride directly react, the materials are flushed into water for separation, filtering and drying are carried out, and prednisolone acetate is prepared.
The technical prejudice that in the prior art of the reaction process, pyridine or a pyridine-substituted solvent is generally used is overcome, the lot production capacity of a reaction still is greatly improved, and it is avoided that a large amount of industrial waste water hard to treat is generated.
The process is simple in process, beneficial to environmental protection, low in cost and suitable for industrial large-scale production. A kind of preparation technology of prednisolone acetate Technical field.
The invention belongs to chemical pharmacy field, and in particular to a kind of preparation technology of prednisolone acetate chemosynthesis. Prednisolone acetate is glucocorticoid medicine, can be used for outward treating anaphylaxis, non-infectious dermatosiss and some hypertrophy Property dermatopathy, it can also be used to treat anaphylaxis and autoimmune inflammation disease, collagenosis etc..
Prednisolone acetate is The important intermediate of synthesis prednisolone and other steroid drugss, in steroid drugss field using extremely wide. Chinese patent CN Chinese patent CN In 3 and 20 deprotection reactions of critical process, conventional fabrication techniques be prior to The system of sodium nitrite solution and hydrochloric acid solution carries out reaction and obtains nitrous compound, then carries out resin hydrolyzing and be further purified removal Prednisolone is obtained after impurity.
Why the deprotection reaction mode combined using nitrosation and resin hydrolyzing, is due to strong It is stronger to the destruction of steroidal ring structure under acid condition, need by adding the reactive mode removal nitrosation of resin hydrolyzing anti- Should during a large amount of impurity for producing and improve product appearance. But still need in deprotection reaction To carry out under strong acid system, it is impossible to avoid destruction and solution loss to steroidal ring structure under strong acidic condition.
Prednisolone adopts pyridine as solvent and the catalyst of reaction with the traditional handicraft of acetic anhydride esterification. Chinese patent So can not only produce substantial amounts of Industrial wastewater, and cannot can bring the solution loss of product with avoiding. Due to the stable chemical nature of DMF and DMSO, it is difficult to Degraded with conventional biological processes, it is necessary to waste water is processed using expensive membrane separation technique, quantity of wastewater effluent is still suffered from excessive, industrial The deficiencies such as cost for wastewater treatment height.
The present invention is directed to the deficiencies in the prior art, there is provided a kind of preparation technology of prednisolone acetate. What the present invention was provided Method significantly reduces the consumption of liquid supplementary material in reaction system, and product yield is high, and amount of industrial wastewater is greatly decreased, and effectively drops Low cost of material and environmentally friendly cost, are adapted to industrial scale production.
It is not required to increase solvent in addition using present invention process, not only significantly carries The high batch production capacity of reactor, and generation is avoided because solvent is using bringing a large amount of reluctant industrial wastewaters, keep away The strip loss of solvent in last handling process is exempted from.
Present invention process has technical process simple, is conducive to environmental conservation, cost Advantage that is low, being suitable for industrialized great production.
For purposes of simplicity and clarity, the description of known conventional production process is hereafter rightly eliminated, in order to avoid those Unnecessary details affects the description to the technical program. The present invention is illustrated with example below, these examples are intended to the technological means for helping understand the present invention. But It should be understood that these embodiments are exemplary, this is the invention is not limited in.
TLC shows that reaction is complete, reactant liquor is poured into and be cooled in DEG C of frozen water in advance, stirs 30 points Zhong Hou, stands more than 2 hours, filters, is dried to obtain 33g prednisolone acetates, HPLC purity TLC shows that reaction is complete, reactant liquor is poured into and be cooled in DEG C of frozen water in advance, stirs 30 points Zhong Hou, stands more than 2 hours, filters, is dried to obtain TLC shows that reaction is complete, reactant liquor is poured into and be cooled in DEG C of frozen water in advance, stirring 30 After minute, more than 2 hours are stood, filter, be dried to obtain CNA en.
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