- PROCESS FOR THE PREPARATION OF VALACYCLOVIR HYDROCHLORIDE
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The present invention provides a process for the preparation of 2-[(2-amino-1,6-dihydro-6-oxo-9H-yl)]ethyl L-valine ester hydrochloride (valacyclovir hydrochloride) of formula I comprising deprotection of N-[(benzyloxy)carbonyl]-L-valine-2-[(2-amino-1,6-dihydro-6-oxo-9H-purin-9-yl)methoxy]ethyl ester, of formula II using 5% palladium on carbon as a catalyst and mineral acid in the presence of water, avoiding use of organic solvents under hydrogen pressure to yield valacyclovir hydrochloride having yield of ≧90% and purity of ≧99.5%, pharmaceutically acceptable grade. The valacyclovir hydrochloride obtained using the process of the present invention is valacyclovir hydrochloride polymorphic Form I.
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Paragraph 0040
(2014/10/16)
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- An efficient and large scale process for synthesis of valacyclovir
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A facile, commercially viable and large scale process is developed for an antiviral drug substance, valacyclovir hydrochloride. Several process related critical factors including organic and heavy metal impurities are efficiently addressed in this process.
- Prasada Raju,Vedantham, Ravindra,Khunt, Mayur D.,Mathad, Vijayavitthal T.,Dubey, Pramod K.,Chakravarthy, Akula Kalyan
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experimental part
p. 4092 - 4098
(2010/11/05)
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- VALACYCLOVIR PROCESS
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A process for preparing valacyclovir or a salt thereof.
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Page/Page column 1; 5-6
(2010/11/27)
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- Method for preparing amino acid esters of nucleoside analogues
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Describes a process for preparing esters of nucleoside analogues comprising condensing a nucleoside analogue with a protected amino acid in the presence of a tertiary amine and in the presence of an activating amount of an activating agent chosen from org
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Page/Page column 5
(2008/06/13)
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- USE OF VALACICLOVIR FOR THE MANUFACTURE OF A MEDICAMENT FOR THE TREATMENT OF GENITAL HERPES BY A SINGLE DAILY APPLICATION
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The invention relates to the antiviral drug valaciclovir, the valine ester of 9-[(2-hydroxyethoxy)methyl]guanine (aciclovir), which is known as an effective treatment for genital herpes in a dosage regime of 40 mg, twice to 5 times daily. More specificall
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- Transport of acyclovir ester prodrugs through rabbit cornea and SIRC-rabbit corneal epithelial cell line
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The purpose of this study is to assess the permeability of acyclovir (ACV) prodrugs through the rabbit corneal cell line (SIRC) as well as the cornea, and characterize the SIRC cell line for transport and metabolism studies of ester prodrugs. Prodrug derivatization of an acycloguanosine antiviral agent, acyclovir, was employed to improve its permeability across the cornea. New Zealand albino rabbits were used as an animal model for corneal studies. The SIRC cell line grown on polyester membranes was used for transport of these prodrugs. SIRC cells grown on the membrane support for 10 days developed four to six layers of epithelial cells, and this is comparable to the normal rabbit corneal epithelial layer. Transport experiments were conducted across the rabbit cornea and confluent SIRC cells using side-by-side diffusion-cell apparatus. Enzymatic hydrolysis of these compounds was evaluated in SIRC cell lysates. Appropriate reversed phase HPLC method(s) were employed for quantitation of both the prodrug and ACV simultaneously. Corneal permeabilities of some of these prodrugs (Malonyl ACV and Acetyl ACV) were higher relative to ACV. The SIRC cell line permeability values of all the prodrugs were higher compared to that of the intact cornea. The total amount of ACV-prodrugs transported, i.e., unhydrolyzed prodrugs and regenerated ACV, across the SIRC cell line was more relative to ACV. Hydrolytic studies in the SIRC cell line homogenate demonstrated the bioreversion potential of the prodrugs and the presence of enzymes, particularly the cholinesterase in the SIRC cell line. It may be concluded that the SIRC cell line is leakier compared to the cornea. Keeping in mind the limitations, the SIRC cell line after further characterization may be used for transport and metabolism studies of ester prodrugs.
- Tak, Rahul V.,Pal, Dhananjay,Gao, Hongwu,Dey, Surajit,Mitra, Ashim K.
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p. 1505 - 1515
(2007/10/03)
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- Process for the production of nucleic acid base derivatives
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[Abstract]Provided is a process which is industrially useful for producing an ester of an amino acid and a nucleoside having a pseudo-sugar moiety. [Structure]A process for the production of an ester of an amino acid and a nucleoside having a pseudo-sugar
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