Lamivudine Salicylate CAS 173522-96-8 For Effective Antiviral Treatment

Product Description:

Product Name: Lamivudine salicylate CAS NO: 173522-96-8

Synonyms:

2r-(Hydroxymethyl)-5(S)-Cytosin-1-Yl-1,3-Oxathiolanesalicycic Acid Salt;

2R-(hydroxymethyl)-5(s)-cytosin-1-yl-[1,3]-oxathiolane salicylic acid salt (intermediate of lamivudine);

Chemical & Physical Properties:

Appearance: White to off-white to light yellow powder

Assay :≥99.00%

Exact Mass: 367.083801

Melting Point: 138-143℃

Safety Information:

Signal Word: Warning

Hazard Statements: H315; H319; H335

Precautionary Statements: P261; P264; P271; P280; P302+P352; P304+P340; P305+P351+P338; P312; P321; P332+P313; P337+P313; P362; P403+P233; P405; P501

Lamivudine is a kind of pharmaceutical raw material with good antiviral activity, which is mainly used for anti-hepatitis B and anti-HIV. It is the main active ingredient in the current cocktail therapy for hepatitis B and AIDS. Its synthesis requires excessive synthesis of intermediates. Lamivudine intermediate HDMS lamivudine salicylate molecular formula: C15H17O6n3S.H2O, its chemical name: (2R-cis) -4-amino-1 -(2-hydroxymethyl-1, 3-oxythiacyclo-pent-yl) -1H-pyridine - 2-ketone salicylate. In the process of lamivudine intermediate synthesis, domestic and foreign public reports. The route published by the United States patent is to use 2-bromodiethoxyethane as raw material, react with thiobenzoic acid and then hydrolysis with sodium hydroxide to obtain 2-chemicalbook diethoxyethane, react with benzoyl oxy acetaldehyde to obtain 2-benzoyl oxy methyl 5-ethoxy-1, 3-oxy thiacyclopentane, then catalyze with trifluoromethylate trimethyl silane. Reaction with cytosine protected by trimethylsilane, acetylation, column chromatography to remove the trans body, deacetylation to obtain the cis product; Acetylation of cis product formic acid and chlorine menthol ester reaction, recrystallization isolated (2 r, 5 s) isomer, ammonia solution for lamivudine, the method 2 to ryukyu and base 2 ethoxy ethane reaction with benzoyl oxygen acetaldehyde to 2 - methyl benzoyl oxygen - 5 - ethoxy - 1, 3 - oxygen heterocyclic sulfur pentane the reaction yield is low, raw materials for complex, also need to remove trans body, The result is that the yield is greatly reduced, the cost is increased, and the use of chromatography column is not conducive to industrial production.

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