764659-72-5Relevant articles and documents
Synthesis of (±)-Emtricitabine and (±)-Lamivudine by Chlorotrimethylsilane-Sodium Iodide-Promoted Vorbrüggen Glycosylation
Jamison, Timothy F.,Mear, Sarah Jane,Nguyen, Long V.,Rochford, Ashley J.
, (2022/02/07)
By simple combination of water and sodium iodide (NaI) with chlorotrimethylsilane (TMSCl), promotion of a Vorbrüggen glycosylation en route to essential HIV drugs emtricitabine (FTC) and lamivudine (3TC) is achieved. TMSCl-NaI in wet solvent (0.1 M water)
Preparation method of emtriva
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Paragraph 0047; 0048; 0049, (2017/08/28)
The invention discloses a preparation method of emtriva. The preparation method comprises following steps: step A, in an alcoholic solvent I, an emtriva crude product and a halogen hydride are subjected to salt forming reaction so as to obtain a emtriva halogen acid salt, wherein the HPLC purity of the emtriva crude product is controlled to be 85.0% or higher, the halogen hydride is selected from hydrogen chloride, hydrogen bromide, or hydrogen iodide, and X is used for representing chlorine, bromine, or iodine; and step B, in an alcoholic solvent II, the emtriva halogen acid salt prepared in step A and an organic alkali are subjected to neutralization reaction so as to obtain emtriva, wherein X is used for representing chlorine, bromine, or iodine. The preparation method is simple in operation, simple in postprocessing, and high in yield; the purity of prepared emtriva is high; HPLC purity is higher than 99.60%; the content of the maximum single impurity is less than 0.10%; bulk pharmaceutical chemical standards are satisfied; production cost is low; and the preparation method is suitable for industrialized production.
PROCESS FOR PRODUCING LAMIVUDINE AND EMTRICITABINE
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Page/Page column 19; 20; 21; 22, (2018/01/20)
This invention provides for flow and batch synthesis processes for the production of Lamivudine and Emtricitabine, including flow and batch synthesis processes wherein at least of the synthesis steps are conducted in a solvent free environment.