- Synthesis and properties of S-phosphates of some antiviral acyclonucleosides
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Suitably protected penciclovir, ganciclovir and 9-[3-hydroxy-2- (hydroxymethyl)propoxy]guanine were converted into their iodo-derivatives which in turn were reacted with trisodium thiophosphate to give the corresponding S-phosphates in good yields.
- Harnden,Serafinowska
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- Synthesis method of high-purity monoacetyl ganciclovir
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The invention discloses a synthesis method of high-purity monoacetyl ganciclovir, comprising the following steps: by taking ganciclovir as material, protecting an alcoholic hydroxyl group with trioctadecyl borate, then adding an acetylation reagent to perform selective acetylation, so as to obtain monoacetyl ganciclovir. The preparation method disclosed by the invention is high in material conversion rate, and good in acetylation selectivity, and the content of the obtained monoacetyl ganciclovir reaches 99% or above, and therefore, the synthesis quality of subsequent valganiclovir products isimproved, the production efficiency is high, and the method is suitable for industrial production.
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Paragraph 0029; 0036; 0038; 0052
(2018/09/08)
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- Method for preparing high-purity mono-acetyl ganciclovir
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The invention discloses a method for preparing high-purity mono-acetyl ganciclovir. The method includes steps of carrying out dibutyltin oxide protection on ganciclovir and alcoholic hydroxyl groups;adding products into acetylation reagents and carrying out selective acetylation; carrying out treatment to obtain the mono-acetyl ganciclovir. The ganciclovir is used as a raw material. The method has the advantages that the method is high in raw material conversion rate and good in acetylation selectivity, and the content of the mono-acetyl ganciclovir prepared by the aid of the method can reach99% at least; the synthesis quality of subsequent valganciclovir products can be improved, and the method is high in production efficiency and suitable for large-scale industrial production.
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Paragraph 0029; 0035; 0036; 0038; 0052
(2018/09/08)
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- A high-purity single-acetyl ganciclovir preparation method (by machine translation)
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The invention discloses a high-purity single-acetyl ganciclovir preparation method, comprises the following steps: to ganciclovir as raw materials, by the sulfite to protect the hydroxyl; subsequently adding acetylation reagent selective acetylation, get mono acetyl ganciclovir. The invention discloses the preparation method of the high conversion rate of raw materials, acetylation good selectivity, obtained list acetyl ganciclovir content of 99% or more, to improve the follow-up [...] absorbable synthetic quality of such products, high production efficiency, and is suitable for large-scale industrial production. (by machine translation)
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Paragraph 0028-0031; 0035-0040; 0046; 0047; 0051-0054
(2018/10/04)
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- Method for synthesizing high-purity monoacetyl ganciclovir
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The invention discloses a method for synthesizing high-purity monoacetyl ganciclovir. The method comprises the following steps: taking ganciclovir as the raw material, using alkyl methoxyl silicon toprotect double hydroxyls of alcoholic hydroxyl group of the raw material, adding an acetylation agent to selectively acetylate, and obtaining the monoacetyl ganciclovir after the processing. The disclosed preparation method is high in conversion rate of the raw material and good in acetylation selectivity, the content of the prepared monoacetyl ganciclovir is 99% or more, the synthesis quality ofthe subsequent valganciclovir product is improved, the production efficiency is high, and the method is suitable for large-scale industrial production.
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Paragraph 0028-0031; 0036-0039; 0047; 0048; 0052-0055
(2018/10/04)
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- High-purity ganciclovir monoacetate preparation method
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The invention discloses a high-purity ganciclovir monoacetate preparation method which comprises the following steps: utilizing ganciclovir as a raw material and protecting alcoholic hydroxyl by methyl boronic acid; then adding an acetylation reagent to perform selective acetylation to obtain ganciclovir monoacetate. The preparation method disclosed by the invention has the advantages of high rawmaterial conversion rate and good acetylation selectivity; a content of the obtained ganciclovir monoacetate can reach 99% or more, synthesizing quality of follow-up valganciclovir products is improved, production efficiency is high, and the preparation method is suitable for large-scale industrial production.
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Paragraph 0029; 0035; 0036; 0038; 0052
(2018/09/11)
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- Synthesis of valganciclovir hydrochloride congeners
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Valganciclovir hydrochloride (1) is used for the treatment of cytomegalovirus (CMV) retinitis in patients with weakened immune systems. Valganciclovir hydrochloride is a hydrochloride salt of L-valyl ester of ganciclovir (2) that exists as a mixture of two diastereomers. According to the U.S. Food and Drug Administration specifications, the diastereomeric ratio of valganciclovir hydrochloride 1 should be maintained in the range 55:45 to 45:55. According to the U.S. Food and Drug Administration specifications, the diastereomeric ratio of valganciclovir hydrochloride 1 should be maintained in the range 55:45 to 45:55. During the process development of valganciclovir hydrochloride, six related substances (impurities) were observed along with the final active pharmaceutical ingredient. Among these six impurities, ganciclovir (2) and guanine (3) are the key starting materials and degraded impurities of ganciclovir, respectively. The remaining four impurities were identified as isovalganciclovir hydrochloride (4), methoxymethylguanine (5), O-acetoxy ganciclovir (6), and isovalarylganciclovir (7). The present work describes the synthesis and characterization of these four impurities.
- Babu, K. Srihari,Rao, M. Raghavendar,Goverdhan,Srinivas,Reddy, P. Pratap,Venkateswarlu,Anand, R. Vijaya
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p. 1751 - 1758
(2013/05/22)
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- Preparation of valganciclovir
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A process for the preparation of valganciclovir with triacetyl ganciclovir (V) as a starting material, comprising the following steps: selective hydrolysis, reacting with a coupling agent and a solvent, followed by hydrolysis under basic conditions and hydrogenolysis in the presence of a catalyst.
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Page/Page column 10-11
(2008/06/13)
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- Preparation of ester of purine derivatives
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A process for the preparation of valganciclovir with triacetyl ganciclovir (V) as a starting material, comprising the following steps: selective hydrolysis, reacting with a coupling agent and a solvent, followed by hydrolysis under basic conditions and hydrogenolysis in the presence of a catalyst.
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Page/Page column 7
(2008/06/13)
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- NMR spectral data for ester prodrugs of ganciclovir
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A series of 9-[(1,3-dihydroxy-2-propoxy)methyl]guanine mono- and diesters, 2a-i, 3a-d and 4a-d, were synthesized as potential prodrugs of ganciclovir and both 1H NMR and 13C NMR spectra were assigned to these esters based on spectral comparison with compounds of similar structure. Copyright
- Gao, Hongwu,Mitra, Ashim K.
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p. 696 - 700
(2007/10/03)
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