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CAS号3012-37-1 硫氰酸苯甲酯 | CAS号100-44-7 氯化苄 | CAS号79-19-6 硫代氨基脲 | CAS号57216-15-6 benzyl N'-amino...合成工艺路线路线简述
- 合成目标产物 5-Benzylthio-1H-Tetrazole 主要起始原料 Benzyl Thiocyanate
- (文献来源)合成步骤主要原料 Benzyl Thiocyanate
硫氰酸苄酯置于sodium Azide,Cerium(III) Chloride Heptahydrate体系中,用 水,异丙醇 用作溶剂,化学反应 4.0H,以47%的收率获得5-苄硫基四氮唑
参考文献:杂芳基,乙烯基,苄基和烷基四唑化合物的抗菌评估
标题:杂芳基,乙烯基,苄基和烷基四唑化合物的抗菌评估
摘要:背景:在以前的报道中,已经描述了某些四唑衍生物的抗菌性能.先前我们已经报道了芳基1Htetrazole化合物的抗菌性能. 目的:研究5-取代的杂芳基,乙烯基,苄基和烷基1H-四唑衍生物的抗菌活性. 方法:研究了杂芳基,乙烯基,苄基和脂肪族四唑衍生物对大肠杆菌,金黄色葡萄球菌和铜绿假单胞菌的抗菌性能.通过确定这些四唑衍生物的最小抑菌浓度并将其与已知的抗生素阿莫西林,甲氧苄啶和磺胺甲恶唑进行比较,来评估活性. 结果:在微波反应器中,使用含水溶剂混合物,在160oc下氯化七水合氯化铈(III)催化1-4小时,制备了四唑化合物.活性最高的衍生物对大肠杆菌的最小抑菌浓度值在125-250 µg / Ml之间.更重要的是,这些化合物与甲氧苄氨嘧啶联用时具有明显更高的活性,并观测到了对大肠杆菌和金黄色葡萄球菌的显着协同作用(mic = 0.98-7.81 µg / Ml). 结论:四唑衍生物在水中的合成
Doi:10.2174/1573406413666171120162420
专利信息
专利号:US-2025313590-A1
优先权日:2024-03-16
标题:Phosphoramidite morpholino monomers towards synthesis/convergent synthesis of PMO, TMO, their chimera oligos in 5 prime to 3 prime direction
发明人:SINHA SURAJIT; GHOSH ATANU; BANERJEE ARPAN
权利人:INDIAN ASS FOR THE CULTIVATION OF SCIENCE
摘要:The present invention relates to 5′-morpholino amidite monomers as 5′-CE/5′- t Bu phosphoramidite morpholino monomers (2) and process chemistry for the efficient synthesis of N-Trityl or monomethoxytrityl (MMTr)-protected 5′-morpholino amidite monomers and their use in the synthesis of phosphorodiamidate morpholino oligonucleotides (PMO), thiophosphoramidate morpholino oligonucleotides (TMO) and their chimeras which can be used for antisense technology or in general oligonucleotides related research.
专利号:WO-2025044766-A1
优先权日:2023-08-31
标题:Use of silicon dioxide microspheres in synthesis of ultra-long oligonucleotide and method for synthesizing ultra-long oligonucleotide
发明人:SHI YONGYONG; ZHANG MANCANG; WANG LIBING; GAO PANPAN; FANG JUN
权利人:UNIV SHANGHAI JIAOTONG; SHANGHAI DYNEGENE TECH CO LTD
摘要:The present invention relates to the technical field of oligonucleotide synthesis. Disclosed are the use of silicon dioxide microspheres in the synthesis of an ultra-long oligonucleotide and a method for synthesizing an ultra-long oligonucleotide, wherein the silicon dioxide microspheres have a specific surface area of less than 1 m2/g, and preferably, the silicon dioxide microspheres have modification groups on the surface. The method for synthesizing an ultra-long oligonucleotide comprises: performing a coupling reaction on a nucleoside phosphoramidite synthesis unit using the silicon dioxide microspheres having modification groups on the surface as carriers under coupling reaction conditions. The prepared carriers can be used to prepare an ultra-long oligonucleotide.
专利号:US-10167308-B2
优先权日:2013-09-14
标题:Highly efficient synthesis of long RNA using reverse direction approach
发明人:SRIVASTAVA SURESH C; SRIVASTAVA NAVEEN P
权利人:CHEMGENES CORP
摘要:The present invention relates to novel process of reverse 5′→3′ directed synthesis of RNA oligomers in the range of about 100-mer to about 200-mer has been developed and disclosed. Using that method demonstrated high quality RNA synthesis with coupling efficiency approaching 99%.
专利号:US-10730904-B2
优先权日:2012-11-14
标 题:Method for liquid-phase synthesis of nucleic acid
发明人:NONOGAWA MITSURU; NAGATA TOSHIAKI; SAITO HIDEKI; YASUMA TSUNEO
权利人:TAKEDA PHARMACEUTICALS CO
摘要:In this method, an oligonucleotide represented by formula (II) [wherein Y 1 , Q, Base, r and r′ are each as defined in claim 1 ] is prepared by using, as a synthesis unit, a novel nucleoside monomer compound represented by formula (I) [wherein X, R 1 , Y, Base, Z, Ar, R 2 , R 3 and n are each as defined in claim 1 ]. The novel nucleoside monomer compound is a nucleoside, the base moiety of which is substituted with an aromatic-hydrocarbon-ring-carbonyl or -thiocarbonyl group having at least one hydrophobic group. The method can dispense with column-chromatographic purification in every reaction, and enables base elongation not only in the 3′-direction but also in the 5′-direction, thus attaining efficient liquid-phase mass synthesis of an oligonucleotide.
专利号:US-2025282813-A1
优先权日:2021-04-09
标 题 :Pseudo solid phase protecting group and methods for the synthesis of oligonucleotides and oligonucleotide conjugates
发明人:OKADA YOHEI; SUZUKI HIDEAKI; LUTHER ANATOL
权利人:BACHEM HOLDING AG
摘要:A novel pseudo solid phase protecting group and methods for the synthesis of oligonucleotides and oligonucleotide conjugates are provided. The pseudo solid phase protecting group is represented by formula II wherein: * indicates the point of attachment to an oxygen atom of a hydroxyl moiety of the nucleoside, the nucleotide, the oligonucleotide, or of the conjugate of a nucleoside, a nucleotide or an oligonucleotide to be protected; c is 0 or 1; a is an integer of 1 to 12; R3 is H; R5 is O—R6 or H, where R6 is a C8-C40 aliphatic hydrocarbon group; each of R4 is independently O—R6, where R6 is at each occurrence independently a C8-C40 aliphatic hydrocarbon group; b is 1 to 3; with the proviso that if b is 1, at least one of R3 and R5 is not H; and with the further proviso that the sum of all carbon atoms contained in the R3, R4, and R5 moieties present is larger than 23 and smaller than 200.
专利号:US-12139507-B2
优先权日:2018-05-02
标题 :Segment for use in synthesis of oligonucleotide, method for producing the same, and method for synthesizing oligonucleotide using the same
发明人:KATAOKA MASANORI
权利人:NATIAS INC
摘要:A segment for use in synthesis of an oligonucleotide, represented by the following formula (I), a method for producing the same, and a method for synthesizing an oligonucleotide therefrom are provided. In formula (I), B is a protected/unprotected nucleoside base; R1 is a protecting group; R2, R3 and R4 are OCH2CH2CN, OCH2CHâ•?CH2, etc.; R5 is a substituted/unsubstituted aliphatic group/aromatic group; X is a lone pair, O or S; Y is NHR6, a halogen, CN, etc., or a hydroxyl group protected with an acyl, ether or silyl protecting group; R6 is H, an aliphatic group or an aromatic group; Z is H, an alkyl, an O- or N-alkyl or a halogen, or forms a Z-Y bond with Y; and (m+n) is an integer of 2 or more and 23 or less.