Paracetamol Lamivudine Raw Materials Powder

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Lamivudine Powder Usage and Synthesis.

Lamivudine is metabolised in HBV-infected and normal cells to produce lamivudine triphosphate, the active form of lamivudine, which is both an inhibitor of HBV polymerase and a substrate for this polymerase.

Lamivudine triphosphate is incorporated into the viral DNA strand, blocking viral DNA synthesis, and does not interfere with normal cellular deoxynucleoside metabolism, with weak inhibition of mammalian DNA polymerases α and β, and virtually no effect on mammalian cellular DNA content. There is no obvious toxicity to the structure, DNA content and function of mitochondria.

The results of serum HBV-DNA testing of most patients with hepatitis B show that lamivudine rapidly inhibits HBV replication, and its inhibitory effect persists throughout the course of treatment. At the same time, serum aminotransferases were reduced to normal, and long-term use of lamivudine can significantly improve the necroinflammatory changes in the liver and reduce or prevent the progression of liver fibrosis.

Uses and functions of Lamivudine.

Antiviral drug used in the treatment of hepatobiliary diseases, hepatitis B, chronic hepatitis B with replication of the hepatitis B virus.

Lamivudine is a nucleoside analogue, whereas nucleotides are the raw materials for the synthesis of DNA and RNA, the genetic material of the human body (DNA and RNA are actually made up of many nucleotides lined up hand in hand in a long string).

Nucleoside analogues mimic the structure of nucleotides structurally, but do not have the function of nucleotides. Therefore, during DNA synthesis, nucleoside analogues can be incorporated, but they cannot synthesise normally functioning nucleic acid strands, thus terminating viral replication. Lamivudine mimics cytosine, which has a different structure from the natural human cytosine structure, and he can only act on viruses without side effects on the human body.

Lamivudine, as a new nucleoside analogue, is widely accepted by doctors and patients, and is a representative nucleoside analogue with good efficacy in clinical application. Its mechanism of action is the inhibition of viral DNA polymerase and reverse transcriptase activity, and competitive inhibition of viral DNA strand synthesis and extension.

Pharmacological Effects of Lamivudine Raw Materials.

Lamivudine is a nucleoside antiviral agent that strongly inhibits hepatitis B virus (HBV) in vitro and in experimentally infected animals.

Lamivudine is metabolised in HBV-infected and normal cells to form lamivudine triphosphate, the active form of lamivudine, which acts as both an inhibitor of HBV polymerase and a substrate for this polymerase. Lamivudine triphosphate is incorporated into the viral DNA strand and blocks the synthesis of viral DNA.

Lamivudine triphosphate does not interfere with normal cellular deoxynucleoside metabolism, and it weakly inhibits mammalian DNA polymerases α and β, with little effect on mammalian cellular DNA content. Lamivudine has no significant toxicity to mitochondrial structure, DNA content or function.

Serum HBV DNA testing of most patients with hepatitis B showed that lamivudine rapidly inhibited HBV replication, and its inhibitory effect persisted throughout the course of treatment.

At the same time, serum aminotransferases were reduced to normal, and long-term use of lamivudine can significantly improve the necroinflammatory changes in the liver and reduce or prevent the progression of hepatic fibrosis.

Production method of Lamivudine Raw Powder.

Selective 6-O-sulfonylation of compound (I) followed by acetylation gave compound (II) in 96.7% yield. Compound (II) was reacted with acetic acid as solvent and 3 moL of hydrogen bromide/L acid (45%, W/V) and brominated to give compound (III) in 99% yield. Bromide (III) and 3.3 moI. potassium salt of ethyl xanthate, refluxed in acetone, were thiolated and cyclised; hydrolysis was then carried out in methanol with ammonia to give compound (IV) in 72% two-step yield.

Compound (IV) was purified by column chromatography as a crystalline solid. Compound (IV) was treated with 1.4 moles of sodium periodate to ring-open the 2,3-cis diol; followed by reduction of the aldehyde formed with sodium borohydride and protection of the diol with the formation of a ketal condensate to give compound (V) in 60% yield. Compound (V) was silylated to protect the remaining primary alcohol, and then the ketal was removed to give compound (VI) in 63% yield.

Lead tetraacetate was used to oxidise the diol in compound (VI), and then the pyridine dichromate layered salt was used to further oxidise the diol, to obtain compound (VII), the oxidation method would not affect the sulphur.

Compound (VII) was further oxidised with lead tetraacetate to obtain compound (VIII) in 66% yield [as compound (VI)]. Compounds (VIII) and (IX), in dichloroethane, were condensed using TMSOTf as Lewis acid catalyst to give compound (X) in 64% yield.

There were also isomers of compound (X) in half the amount of compound (X), which could be separated by silica gel chromatography. Compound (X) was deacetylated with ammonia-methanol in 73% yield and desilanated with tetrabutylammonium fluoride to give lamivudine in 75% yield.

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