57375-25-4

Usage

Uses

3-Bromorifamycin S is a derivative of Rifamycin (R508200), an antibacterial agent.

InChI:InChI=1/C37H44BrNO12/c1-15-11-10-12-16(2)36(47)39-27-26(38)31(44)23-24(32(27)45)30(43)20(6)34-25(23)35(46)37(8,51-34)49-14-13-22(48-9)17(3)33(50-21(7)40)19(5)29(42)18(4)28(15)41/h10-15,17-19,22,28-29,33,41-43H,1-9H3,(H,39,47)/b11-10+,14-13+,16-12+

Upstream product

• 62623-68-1 rifamycin S 
• 6998-60-3 rifamycin SV 

Downstream Products

• 113102-19-5 2'-(N,N-diethylamino)rifamycin P 
• 123812-42-0 16,17,18,19-tetrahydro-3-rifamycin SV 
• 123812-43-1 16,17,18,19,28,29-hexahydro-3-rifamycin SV 
• 62041-01-4 3-amino-4-imino-rifamycin S 
• 96165-99-0 C₄₉H₅₅N₃O₁₂ 
• 80621-81-4 rifaximin 
• 109006-01-1 3-rifamycin SV 

Relevant academic research and scientific papers

Rifaximin hapten and rifaximin artificial antigen, and preparation methods and application thereof

The invention discloses a rifaximin hapten and a rifaximin artificial antigen, and a preparation method and application of the rifaximin hapten and the rifaximin artificial antigen. The rifaximin artificial antigen provided by the invention is an antigen obtained by coupling the rifaximin hapten shown as a formula I which is described in the specification with a carrier protein. The rifaximin artificial antigen provided by the invention is simple in synthesis method, high in purity and high in yield, and has important value for preparation of a rifaximin antibody and detection of rifaximin drug residues.

PROCESS FOR THE PREPARATION OF RIFAXIMIN CRYSTALLINE FORM

The present invention relates to an improved process for the preparation Crystalline Form G2 of Rifaximin of Formula (I). The invention also relates to crystalline Form G2 of Rifaximin (I) obtained by the process of the present invention, the said Form G2 being substantially pure, stable and characterized by X-ray powder diffraction pattern comprising peaks selected from 5.3, 5.7, 6.4, 6.9, 7.1, 7.7, 8.7, 10.4, 10.5, 11.0, 1 1.5, 1 1.8, 17.2, 17.6, 18.2, 18.5 and 20.9 ± 0.2° 2θ. The invention also relates to crystalline Form Gl of Rifaximin (I) obtained by the process of the present invention, the said Form Gl being substantially pure, stable and characterized by X-ray powder diffraction pattern comprising peaks selected from 5.4, 6.6, 7.4, 7.9, 8.8, 10.5, 1 1.0, 1 1.8, 12.9, 17.6, 18.5, 19.7, 21.0, 21.4, 22.1 ± 0.2° 2θ.. The present invention further relates to process for the preparation of substantially pure Rifaximin comprising recrystallization in alcohol or in mixture of water and alcoholic solvents.

AN IMPROVED PROCESS FOR THE PREPARATION OF RIFAMYCIN DERIVATIVES

The present invention relates to an improved and industrially advantageous process for the preparation of Rifaximin with high purity and yield. Particularly, the present invention relates to improved processes for the preparation of Rifaximin from Rifamycin O and S. More particularly the present invention relates to a process for the preparation of Rifaximin through 3-halorifamycin S. The present invention further relates to a novel polymorph of Rifaximin and process for its preparation.

Preparation method for rifamycin S derivative

The invention relates to a preparation method for a rifamycin S derivative. According to the preparation method, 3-amino-4-imine rifamycin S as shown in a formula II which is described in the specification and a 4-piperidone derivative as shown in a formula III which is described in the specification are added according to a certain feeding mode and subjected to a condensation reaction in the presence of an organic solvent, ammonium acetate and zinc dust so as to produce the rifamycin S derivative as shown in a formula I which is described in the specification. The feeding mode is that the 3-amino-4-imine rifamycin S is added into a reaction system in a final step, so 3-amino-4-imine rifamycin S is prevented from reduction and hydrolysis. The preparation method increases the utilization rate of materials and is shortened in reaction time, so high-efficiency high-yield preparation of the rifamycin S derivative is realized, and the yield and content of the rifamycin S derivative reach 80% or above and 95% or above, respectively; and the preparation method overcomes the problems of long reaction time, low yield, many impurities and high cost, and is simple to operate, highly efficient, environment friendly and beneficial for large-scale production.

RIFAMYCIN DERIVATIVES EFFECTIVE AGAINST DRUG-RESISTANT MICROBES

Rifamycin derivatives having antimicrobial activities, including activities against drug-resistant microorganisms are claimed in this invention. The inventive rifamycin derivatives are uniquely designed in that they have a rifamycin moiety covalently linked to a linker group through the C-3 carbon of the rifamycin moiety and the linker is, in turn covalently linked to a therapeutic moiety or antibacterial agent/pharmacophore. The therapeutic moiety can be a quinolone, an oxazolidinone, a macrolide, an aminoglycoside, a tetracycline core or a structure/pharmacophore associated with an antibacterial agent.