114108-84-8Relevant articles and documents
Truncated phosphonated C-1′-branched N,O-nucleosides: A new class of antiviral agents
Romeo, Roberto,Carnovale, Caterina,Giofrè, Salvatore V.,Romeo, Giovanni,MacChi, Beatrice,Frezza, Caterina,Marino-Merlo, Francesca,Pistarà, Venerando,Chiacchio, Ugo
, p. 3652 - 3657 (2012)
Truncated phosphonated C-1′-branched N,O-nucleosides have been synthesized in good yields by 1,3-dipolar cycloaddition methodology, starting from N-methyl-C-(diethoxyphosphoryl)nitrone 7. Preliminary biological assays show that β-anomers are able to inhibit HIV in vitro infection at concentrations in the micromolar range. Higher SI values with respect to AZT indicated that the compounds were endowed with low cytotoxicity.
Oral Delivery of Propofol with Methoxymethylphosphonic Acid as the Delivery Vehicle
Wei, Yonggang,Qiu, Guanpeng,Lei, Bailin,Qin, Linlin,Chu, Hongzhu,Lu, Yonghua,Zhu, Guozhi,Gao, Qiu,Huang, Qingping,Qian, Guofei,Liao, Pengfei,Luo, Xinfeng,Zhang, Xiaowei,Zhang, Chen,Li, Yao,Zheng, Suxin,Yu, Yan,Tang, Pingming,Ni, Jia,Yan, Pangke,Zhou, Yi,Li, Pan,Huang, Xia,Gong, Aisheng,Liu, Jianyu
, p. 8580 - 8590 (2017)
Phosphonamidate 3a of methoxymethylphosphonic acid (MMPA) with propofol (1) and l-alanine ethyl ester was found to be an efficient scaffold for the oral delivery of compound 1. The synthesis and evaluation of MMPA based phosphonamidates of compound 1, HSK3486 (2), and other phenolic drugs revealed the general application of MMPA as the effective delivery vehicle for phenolic drugs. On the basis of plasma concentrations of compound 1 and SN38 (14), the oral bioavailability of compound 3a and 15 in beagle dogs was found to be 97.6% and 34.1%, respectively.
An efficient synthesis of phosphonate derivatives of 1,2-disubstituted carbocyclic purine nucleosides with a cyclopentane ring
Besada, Pedro,Gonzalez Moa, Maria J.,Teran, Carmen
, p. 2363 - 2368 (2008)
The synthesis of phosphonate 1,2-disubstituted carbocyclic nucleosides with a cyclopentane ring is described following two different strategies: inclusion of the phosphonomethyl group before or after coupling of the carbocyclic moiety with the heterocyclic base. The diethyl [(trifluoromethanesulfonyl)oxy] methanephosphonate is the key phosphonylating agent for both the strategies. Georg Thieme Verlag Stuttgart.
Method of preparing tenofovir
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Paragraph 0064; 0065; 0066, (2017/08/25)
The invention provides a method for preparing tenofovir. The method is characterized by comprising the following steps: 1) reacting 9-(2-hydroxy propyl) adenine with a compound as shown in the formula (1) in the specification in the presence of magnesium alkoxide to prepare tenofovir ethyl ester, wherein Y is selected from methyl, trifluoromethyl, phenyl or 4-trifluoromethylphenyl; 2) hydrolyzing the tenofovir ethyl ester in the presence of a dealkylation reagent to prepare tenofovir. The method for preparing tenofovir provided by the invention has the advantages of safe process, good product quality, high yield and suitability for industrialization.
Improved Method for Preparing (R)-9-[2-(phosphonomethoxy)propyl]adenine
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Paragraph 0072-0075, (2021/06/15)
The present invention relates to a method for preparing high purity (R)-9-[2-(phosphonomethoxy)propyl]adenine (PMPA), According to the present invention, the method uses dialkyl methylsulfonyl-oxymethyl phosphonate, which generates only a small amount of impurities in a reaction and has high purity, as an intermediate to prepare the high purity PMPA with a small amount of impurities. The present invention does not use a reagent sensitive to air and moisture contact to enhance safety and allow reproducible production and is easily handled to enable mass production. The high purity PMPA prepared by using the method can be used to prepare tenofovir disoproxil and acidic salt thereof in order to give a very favorable advantage for the production of high quality drug ingredient.COPYRIGHT KIPO 2016
Synthesis and screening of novel inositol phosphonate derivatives for anticancer functions in vitro
Chen, Wen-Bin,Liu, Jian-Bing,Dou, Dao-Lei,Song, Fan-Bo,Li, Lu-Yuan,Xi, Zhen
, p. 329 - 333 (2015/04/14)
Phosphonates have been frequently used as suitable isosteric and isoelectronic replacements for biologically important phosphates in the development of drugs or drug candidates because of their stability toward the action of phosphatases and other enzymes. In this paper, 12 mono-phosphonate inositol compounds were prepared with phosphonate instead of phosphate by two kinds of strategies, nucleophilic substitution and Arbuzov rearrangement, respectively. All compounds were evaluated in vitro for their activity against non-small cell lung cancer (NSCLC) cell line A549. Two compounds (3ac and 3bb) exhibited good antitumor activity at 10 μg/mL.
Synthesis of 2-phosphono alkyl 1,2-benzisoselenazol-3(2H)-ones
Hu, Liming,Lu, Shengmei,Yang, Fengling,Feng, Juhong,Liu, Zhaojie,Xu, Hansheng,He, Hongwu
, p. 2785 - 2790 (2007/10/03)
A series of 2-phosphonoalkyl 1,2-benzisoselenazol-3(2H)-ones were designed and synthesized via reaction 2-chloroselenobenzoyl chloride with 1-hydrazinobenzyl phosphonate. The structures of all new compounds were confirmed by spectroscopic methods and microanalyses.
Studies of organophosphorus compounds 91: A novel synthesis of 1-hydrazinoalkylphosphonic acids and derivatives thereof
Yuan,Li
, p. 507 - 510 (2007/10/03)
Condensation of diethyl phosphite with aldehydes followed by subsequent sulfonylation of the resulting hydroxy group formed with mesyl chloride gave the corresponding 1-sulfonyloxyalkylphosphonates, which led to the convenient synthesis of 1-hydrazinoalky
