- Antitubercular nanocarrier combination therapy: Formulation strategies and in vitro efficacy for rifampicin and SQ641
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Tuberculosis (TB) remains a major global health concern, and new therapies are needed to overcome the problems associated with dosing frequency, patient compliance, and drug resistance. To reduce side effects associated with systemic drug distribution and
- Daddio, Suzanne M.,Reddy, Venkata M.,Liu, Ying,Sinko, Patrick J.,Einck, Leo,Prudhomme, Robert K.
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- New scavenger resin for the reversible linking and monoprotection of functionalized aromatic aldehydes
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(Chemical Equation Presented) Polymer-supported benzylhydrazines were synthesized using poly(ethylene glycol) acrylamide (PEGA) resin. They can be used to scavenge electrophiles reactive with hydrazine. Especially aromatic aldehydes can be captured select
- Zhu, Mingzhao,Ruijter, Eelco,Wessjohann, Ludger A.
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- Method of purifying rifampicin
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The invention discloses a method for purifying rifampicin. The rifampicin to-be-purified is hydrolyzed into 3-formyl rifamycin SV, the 3-formyl rifamycin SV and hydrosulfite form an alpha-hydroxyl sodium sulfonate structure of rifamycin, impurities are removed, alkali is adjusted to be converted into 3-formyl rifamycin SV, the 3-formyl rifamycin SV and 1-amino-4-methylpiperazine are condensed to obtain a rifampicin crude product, and refining is performed. The unknown single impurities of the rifampicin product obtained by the method are all less than 0.1%.
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Paragraph 0056-0060
(2020/05/01)
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- Process method for synthesizing rifampicin
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The invention relates to a process method for synthesizing rifampicin, wherein the process method mainly comprises the steps: by using rifamycin S as a raw material, carrying out cyclization reactionto obtain a rifamycin oxazine-containing solution, and carrying out solventing-out crystallization on the rifamycin oxazine-containing solution to obtain a rifamycin oxazine crude product; carrying out condensation reaction on the crude rifamycin oxazine product and 1-amino-4-methylpiperazine to obtain a reaction solution containing rifampicin; and cooling and crystallizing the reaction solution containing rifampicin to obtain a rifampicin product. Compared with the prior art, the method has the advantages that the reaction steps are few, the product yield is high, the reaction raw material cost is low, meanwhile, the production is more environmentally friendly, the consumption of raw materials is reduced by 30% (the consumption of dimethylol tert-butylamine required by every 1 kg of rifamycin S is reduced by about 28%, and the consumption of 1-amino-4-methylpiperazine is reduced by about 30%). The method overcomes the defect that a large amount of sewage is generated in production byadopting an elution method, and reduces the influence of impure reaction products on the yield due to the fact that rifamycin S-Na is used as a raw material.
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Paragraph 0059; 0063-0065; 0069-0071; 0075-0077; 0081-0082
(2020/11/24)
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- Method for preparing rifampicin through micro-channel reaction device
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The invention discloses a method for preparing rifampicin through a micro-channel reaction device. Through the micro-channel reaction device, rifamycin S serves as the raw material, and a coarse rifampicin product is directly obtained through the cyclization, hydrolysis, condensation and crystallization process without the after-treatment process. The complete continuity of production of the rifampicin is realized, and the rifampicin is high in yield, low in cost, high in benefit, environmentally friendly, capable of saving energy, high in efficiency and suitable for industrial application.
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Paragraph 0037-0056
(2018/09/29)
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- Method for preparing rifampicin by utilizing cascade reaction of kettle type reaction device and microchannel reaction device
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The invention provides a method for preparing rifampicin by utilizing cascade reaction of a kettle type reaction device and a microchannel reaction device. In the kettle type reaction device, rifamycin S sodium salt is used as a raw material to obtain N-tedin-1,3-oxazine (5,6-C) rifamycin through reaction, and the N-tedin-1,3-oxazine (5,6-C) rifamycin reacts with 1-methyl-4-amino-piperazine in the microchannel reaction device to obtain the rifampicin. Continuous production of the rifampin is achieved, the product quality is good, the cost is low, the profit is high, and the method is green, environmentally friendly, capable of saving energy, efficient and suitable for industrial application.
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Paragraph 0033; 0034; 0043; 0044; 0051-0062; 0065-0068
(2017/08/28)
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- Method for continuous production and preparation of rifampicin from rifamycin S sodium salt
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The invention provides a method for continuous production and preparation of rifampicin from a rifamycin S sodium salt. The continuous production of the rifampicin is achieved by taking rifamycin sodium salt, dihydroxymethyl tert-butyl amine, 1-methyl-4-amino-piperazine as raw materials, and connecting a tank reactor with a microreactor in series. Compared with the prior art, the method provided by the invention achieves continuous production of the rifampicin, the steps of solvent replacement during reaction, solid precipitation and the like are omitted, raw materials and heat energy are greatly saved, the cost is saved, and profits are increased. Meanwhile, according to the method provided by the invention, the characteristics high-efficiency heat transferring capability and easy and direct amplification of a microchannel reactor are utilized, and on the premise that 1/3 of the raw material, namely 1-methyl-4-amino-piperazine, is reduced, the conversion rate of the rifampicin is high and reaches 85% or above, the product quality is good, and the energy consumption is low, so that the method is an environmentally friendly and efficient method for synthesizing the rifampicin, and is suitable for industrial production.
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Paragraph 0028; 0029; 0030; 0031; 0032; 0033-0073
(2017/08/14)
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- Acid and base stable diphenylmethanol derivatives and methods of use
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The invention provides compounds that are useful as linkers for solid phase synthesis and as protecting groups, and methods for producing and using the same.
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Page/Page column 8-9
(2008/12/08)
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- Process and device for producing liquid dosage formulations of medicinal compounds on demand from tablets and capsules
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The present invention provides a process for preparing liquid pharmaceutical formulations on demand from tablets and capsules.
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- AMYLOID BETA-PROTEIN AGGLUTINATION AND/OR DEPOSITION INHIBITOR
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An amyloid β-protein agglutination and/or deposition inhibitor containing rifamycin represented by formula (I) or a pharmaceutically acceptable salt thereof as the active ingredient; and a drug containing the same for treating or preventing senile dementi
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- Process for the preparation of rifampicin
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The present invention provides a process for the preparation of rifampicin, wherein rifamycin S is reacted in an aprotic dipolar solvent with a 1,3,5-trisubstituted hexahydro-1,3,5-triazine at a temperature from 20° to 100° C. followed by reaction with 1-
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- Process for the preparation of 3-iminomethyl derivatives of rifamycin SV
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A process for the preparation in homogeneous phase and in quantitative yield of 3-iminomethyl derivatives of rifamycin SV useful as antibiotic agents. Rifamycin S is reacted in an organic solvent to give a solution of 1,3-oxazino-(5,6-c) rifamycins which
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