Acyclic nucleoside bisphosphonates: synthesis and properties of chiral 2-amino-4,6-bis((phosphonomethoxy)alkoxy)pyrimidines.

Dracínsky Martin; Masojídková Milena; Solínová Veronika; Kasicka Václav; Holy Antonín

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Acyclic nucleoside bisphosphonates: synthesis and properties of chiral 2-amino-4,6-bis((phosphonomethoxy)alkoxy)pyrimidines.

机译：无环核苷双膦酸酯：手性2-氨基-4,6-双（（膦氧基甲氧基）烷氧基）嘧啶的合成和性质。

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2-Amino-4,6-bis[(phosphonomethoxy)alkoxy]pyrimidines bearing two equal or different achiral or chiral phosphonoalkoxy chains have been prepared either by aromatic nucleophilic substitution of 2-amino-4,6-dichloropyrimidine or by alkylation of 4,6-dihydroxy-2-(methylsulfanyl)pyrimidine with appropriate phosphonate-bearing building block. Alkylation of 4,6-dihydroxy-2-(methylsulfanyl)pyrimidine proved to be the method of choice for efficient preparation of variety of bisphosphonates. The enantiomeric purity of selected compounds was determined by capillary electrophoresis. Antiviral activity of bisphosphonates is discussed.

机译：通过2-氨基-4,6-二氯嘧啶的芳族亲核取代或通过烷基化4，可以制备带有两个相同或不同的非手性或手性膦酰基烷氧基链的2-氨基-4,6-双[（膦氧基甲氧基）烷氧基]嘧啶。 6-二羟基-2-（甲基硫烷基）嘧啶，带有适当的膦酸酯基团。 4，6-二羟基-2-（甲基硫烷基）嘧啶的烷基化被证明是有效制备各种双膦酸酯的选择方法。通过毛细管电泳确定所选化合物的对映体纯度。讨论了双膦酸盐的抗病毒活性。

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《European Journal of Medicinal Chemistry: Chimie Therapeutique》 |2009年第6期|共17页
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Dracínsky Martin; Masojídková Milena; Solínová Veronika; Kasicka Václav; Holy Antonín;
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1. Acyclic nucleoside bisphosphonates: synthesis and properties of chiral 2-amino-4,6-bis((phosphonomethoxy)alkoxy)pyrimidines. [J] . Dracínsky Martin, Masojídková Milena, Solínová Veronika, European Journal of Medicinal Chemistry: Chimie Therapeutique . 2009,第6期

机译：无环核苷双膦酸酯：手性2-氨基-4,6-双（（膦氧基甲氧基）烷氧基）嘧啶的合成和性质。
2. The synthesis and antiviral properties of acyclic nucleoside analogues with a phosphonomethoxy fragment in the side chain. [J] . Khandazhinskaya A, Yasko M, Shirokova E Current medicinal chemistry . 2006,第24期

机译：侧链具有膦酰基甲氧基片段的无环核苷类似物的合成和抗病毒特性。
3. The Synthesis and Antiviral Properties of Acyclic Nucleoside Analogues with a Phosphonomethoxy Fragment in the Side Chain [J] . A. Khandazhinskaya M. Yasko and E. Shirokova* Current Medicinal Chemistry . 2006,第24期

机译：侧链具有膦氧基甲氧基片段的无环核苷类似物的合成及抗病毒特性
4. Synthesis of 2-alkoxy-4,6-bis(trinitromethyl)-1,3,5-triazines [C] . Alexandr A. Gidaspov, Vladimir V. Bakharev, Ivan K. Kukushkin, Seminar on New Trends in Research of Energetic Materials;NTREM '10 . 2011

机译：2-烷氧基-4,6-双（三硝基甲基）-1,3,5-三嗪的合成
5. Part I. Asymmetric synthesis of bicyclic analogues of risedronate as molecular probes of the mechanism of action of bisphosphonate antiosteoporotic drugs and potentially more efficacious antiosteoporotic agents. Part II. Facile preparation and functionalization of chiral stabilized ylides from common chiral auxiliaries using the Bestmann ylide and their use in Wittig reactions. Part III. Asymmetric organocatalysis: 1. An investigation of alpha-hydroxylation of aldehydes; 2. Synthesis of a novel camphor-based alpha-aminotetrazole organocatalyst. [D] . Song, Xinyi. 2007

机译：第一部分：利塞膦酸盐双环类似物的不对称合成，作为双膦酸盐类抗骨质疏松药和潜在更有效的抗骨质疏松药作用机理的分子探针。第二部分使用Bestmann内酯从常见手性助剂轻松制备和官能化手性稳定化的叶基及其在Wittig反应中的用途。第三部分不对称有机催化：1.醛的α-羟基化研究； 2.合成新的基于樟脑的α-氨基四唑有机催化剂。
6. Acyclic Nucleoside Bisphosphonates: Synthesis and Properties of Chiral 2-Amino-46-bis(phosphonomethoxy)alkoxypyrimidines [O] . Petra Doláková, Martin Dračínský, Milena Masojídková, -1

机译：无环核苷双膦酸酯：手性2-氨基-46-双（膦氧基甲氧基）烷氧基嘧啶的合成与性质
7. Antischistosomal Activity of Hexadecyloxypropyl Cyclic 9-(S)-[3-Hydroxy-2-(Phosphonomethoxy)Propyl]Adenine and Other Alkoxyalkyl Esters of Acyclic Nucleoside Phosphonates Assessed by Schistosome Worm Killing In Vitro▿ [O] . Botros, Sanaa S., William, Samia, Beadle, James R., 2009

机译：血吸虫蠕虫的体外杀虫作用评估十六烷氧基丙基环9-（S）-[3-羟基-2-（膦氧基甲氧基）丙基]腺嘌呤和其他烷氧基烷基酯的抗血吸虫病活性

Acyclic nucleoside bisphosphonates: synthesis and properties of chiral 2-amino-4,6-bis((phosphonomethoxy)alkoxy)pyrimidines.

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