Synonyms:GS 4071;GS 4104;GS-4071;GS-4104;GS4071;GS4104;Oseltamivir;Tamiflu
99% *data from raw suppliers
Oseltamivir *data from reagent suppliers
There total 195 articles about Oseltamivir which guide to synthetic route it. The literature collected by LookChem mainly comes from the sharing of users and the free literature resources found by Internet computing technology. We keep the original model of the professional version of literature to make it easier and faster for users to retrieve and use. At the same time, we analyze and calculate the most feasible synthesis route with the highest yield for your reference as below:
Reference yield: 100.0%
Reference yield: 98.5%
Reference yield: 98.0%
This research details a novel Azide-Free Synthesis of Oseltamivir, an anti-influenza drug, from L-Methionine. The purpose of the study was to develop an alternative synthesis method that avoids the use of hazardous azide reagents, addressing the safety and availability concerns associated with the commercial production of Oseltamivir, which relies heavily on semisynthesis from less available shikimic acid. The researchers successfully developed a new synthetic pathway that utilizes the Staudinger reaction for the highly enantioselective and stereoselective construction of the three contiguous chiral centers of Oseltamivir. The conclusions highlight the method's advantages of using readily available starting materials, an azide-free synthetic route, and the highly stereoselective construction of the target molecule's chiral centers.
The research focused on the discovery of N-substituted oseltamivir derivatives as potent and selective inhibitors of H5N1 influenza neuraminidase. The study was motivated by the increasing concern of another global flu pandemic, particularly the threat posed by the highly pathogenic avian influenza A (H5N1) virus. The researchers designed and synthesized two series of oseltamivir derivatives targeting the 150-cavity of Group-1 neuraminidase (NA) enzymes, which are especially involved in combating the H5N1 virus. The most potent N1-selective inhibitor among these compounds was compound 20l, with IC50 values of 0.0019 μM, 0.0038 μM, and 0.0067 μM against NAs from three H5N1 viruses, outperforming oseltamivir carboxylate. Another notable compound was compound 32, which exhibited a 12-fold increase in activity against the H274Y mutant relative to oseltamivir carboxylate. The study utilized various chemicals in the synthesis process, including oseltamivir phosphate as the primary starting material, aldehydes for the formation of key intermediates, and reagents such as NaBH3CN, (Boc)2O, and TFA for different synthetic steps. The research also involved the use of 2′-(4-methylumbelliferyl)-α-D-N-acetylneuraminic acid (MUNANA) as a substrate in the neuraminidase inhibition assay to evaluate the inhibitory activities of the synthesized compounds. The findings represent a significant breakthrough in the development of potent Group-1-specific neuraminidase inhibitors, which could be further investigated for the treatment of H5N1 virus infections.
Total 8 Pictures about this product
