CAS: 461-89-2; 1,2,4-Triazine-3,5(2H,4H)-Dione

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[(氨基羰基)亚肼基]乙酸置于sodium Hydroxide体系中,用 乙二醇 作为反应溶剂,以61.6%的收率获得产物6-氮杂脲嘧啶
参考文献:5-Ht1A受体激动剂乙丙哌酮游离碱的改进合成
标题:5-Ht1A受体激动剂乙丙哌酮游离碱的改进合成
摘要:乙哌酮游离碱,F11440,4-甲基-2-(4-(4-(嘧啶-2-基)哌嗪-1-基)丁基)-1,2,4-三嗪-3,5(2H,4H)-二酮,代表一种有效的,选择性的5-Ht1A受体激动剂,具有很高的功效和调节焦虑症的潜力.在本文中,我们报告了一种逆向合成依他普龙游离碱的方法.该化合物由杂环芳族部分和脂族部分组成,合成路线由总共九个步骤组成,从市售材料开始,总收率为8.8%.合成方法的关键步骤包括:(1)使用氢氧化钠和乙二醇作作为反应溶剂,可以得到更好的1,2,4-三嗪-3,5(2H,4H)环化率和产率(61.6%))-Dione; (2)在以三乙胺为碱,乙醇作为反应溶剂,化学反应温度为最优化条件下,得到(嘧啶-2-基)哌嗪-1-甲酸4-叔丁酯的合格产率(63.1%).在非金属催化下,在50oc下放置16小时,副产物更少;(3)以碳酸钾为碱,乙腈作为反应溶剂,Nai为催化剂,反应温度为50oc的条件优化的条件下,
DOI:10.1007/s11696-019-00685-1

专利信息

专利号:US-7229797-B1
优先权日:1999-08-20
标 题:Enzymatic synthesis of deoxyribonucleosides
发明人：TISCHER WILHELM; IHLENFELDT HANS-GEORG; BARZU OCTAVIAN; SAKAMOTO HIROSHI; PISTOTNIK ELISABETH; MARLIERE PHILIPPE; POCHET SYLVIE
权利人:PASTEUR INSTITUT
摘要:The present invention relates to a method for the in vitro enzymatic synthesis of deoxyribonucleosides and enzymes suitable for this method.

专利号:US-6624294-B2
优先权日:1999-01-08
标 题:Regioselective synthesis of 2′-O-modified nucleosides
发明人：KAWASAKI ANDREW M; FRASER ALLISTER S; MANOHARAN MUTHIAH; COOK P DAN; PRAKASH THAZHA P
权利人:ISIS PHARMACEUTICALS INC
摘要:Methods for the regioselective alkylation at the 2'-hydroxy position over the 3'-hydroxy position of nucleosides and nucleoside analogs, forming 2'-O-ester modified compounds, are disclosed. Reduction and derivatization of the 2'-O-ester provides 2'-O-modified nucleosides and nucleoside analogs useful for the synthesis of oligomeric compounds having improved hybridization affinity and nuclease resistance.

专利号:US-4849513-A
优先权日:1983-12-20
标 题 :Deoxyribonucleoside phosphoramidites in which an aliphatic amino group is attached to the sugar ring and their use for the preparation of oligonucleotides containing aliphatic amino groups
发明人：SMITH LLOYD M; FUNG STEVEN; KAISER ROBERT J
权利人:CALIFORNIA INST OF TECHN
摘要:The invention consists of compounds and methods for the synthesis of oligonucleotides which contain one or more free aliphatic amino groups attached to the sugar moieties of the nucleoside subunits. The synthetic method is versatile and general, permitting amino groups to be selectively placed at any position on oligonucleotides of any composition or length which is attainable by current DNA synthetic methods. Fluorescent dyes or other detectable moieties may be covalently attached to the amino groups to yield the corresponding modified oligonucleotide.

专利号:US-5118802-A
优先权日:1983-12-20
标 题:DNA-reporter conjugates linked via the 2' or 5'-primary amino group of the 5'-terminal nucleoside
发明人：SMITH LLOYD M; FUNG STEVEN; KAISER JR ROBERT J
权利人:CALIFORNIA INST OF TECHN
摘要:The invention consists of compounds and methods for the synthesis of oligonucleotides which contain one or more free aliphatic amino groups attached to the sugar moieties of the nucleoside subunits. The synthetic method is versatile and general, permitting amino groups to be selectively placed at any position on oligonucleotides of any composition or length which is attainable by current DNA synthetic methods. Fluorescent dyes or other detectable moieties may be covalently attached to the amino groups to yield the corresponding modified oligonucleotide.

专利号:US-11254958-B1
优先权日:2018-06-20
标 题:Metabolic engineering of E coli with thio-phosphate
发明人：FRAYNE ELIZABETH GAY
权利人:FRAYNE ELIZABETH GAY
摘要:The present invention describes the use of thio-phosphate in the metabolic engineering of E. coli . Thio-phosphate can be used to increase the metabolic flux in important synthetic pathways to enhance the production of bioproducts. The pathways impacted include the following: fatty acid synthesis, isoprenoid syntheses, Vit K2 synthesis, ribonucleotide synthesis, and the synthesis of phosphoribosyl pyrophosphate (PRPP) derivatives like 5-aminoimidazole-4-carboxamide (AICA riboside), histidine, and tryptophan. Thus, thio-phosphate can be used to assist in the production of these molecules and/or their derivatives. Enhanced production of AICA in Bacillus megaterium is also demonstrated.

专利号:WO-2025085030-A1
优先权日:2023-10-18
标 题:Synthesis of semisynthetic penicillin derivatives containing hydrazone-derived thiazolidine and imidazole ring
发明人：SARIPINAR EMIN; BURAN SUMEYYE
权利人:ERCIYES UNIV
摘要:The present invention relates to the novel semi-synthetic thiazolidine and imidazole penicillin, pharmaceutically acceptable derivatives thereof and their synthesis method that may cause biologically significant changes by the N-acylation reaction of 6-aminopenicillanic (6-APA) using new trisubstituted thiazolidine and imidazole acetyl chloride derivatives. The invention also relates to pharmaceutical compositions comprising these compounds and their use for therapeutic treatment in the human or animal body.