Biotage 微波合成仪 Initiator+

Synthesis of [5,6]-fused pyridocoumarins through aza-Claisen rearrangement of 6-propargylaminocoumarins by Biotage Initiator耐士科技

[5,6]-Fused pyridocoumarins are prepared through aza-Claisen rearrangement and subsequent in situ cyclization of 6-propargylaminocoumarins under microwave irradiation in the presence of boron trifluoride diethyl etherate in N,N-dimethylformamide. During this process demethoxycarbonylation is observed in the corresponding 4-carbomethoxycoumarin derivatives.

Synthesis and xanthine oxidase inhibitory activity of 5,6-dihydropyrazolopyrazolo[1,5-c]quinazoline derivatives by Biotage Initiator耐士科技

Some 5,6-dihydropyrazolo/pyrazolo[1,5-c]quinazoline derivatives were rationally designed, synthesized and evaluated for in vitro xanthine oxidase inhibitory activity for the first time. Some notions about structure activity relationships are presented. The compounds 6g, 6h and 6e were found to be significantly active against XO. The compound 6g emerged as the most potent XO inhibitor as compared to allopurinol and free radical scavenger. The molecular docking of 6g into the XO active site highlighted its mode of binding and important interactions such as hydrogen bonding, p–p stacking with amino acid residues like Ser876, Thr1010, Phen914, Phe1009 and Phe649 and its close proximity to dioxothiomolybdenum(MOS).

Synthesis and electro-polymerisation of a novel heteropentalene mesomeric betaine preparation of a novel low band-gap conjugated polymer by Biotage Initiator耐士科技

The 3,4-ethylenedioxythiophene (EDOT)-containing heteropentalene mesomeric betaine 9 has been prepared and electro-polymerised. When coated onto an indium tin oxide (ITO) covered glass slide the optical band-gap of the polymer was determined as 1.75 eV.

Simple conversion of fully protected amino acids to zwitterions by Biotage initiator耐士科技

An operationally simple and efficient method under mild acidic conditions was developed to convert fully protected amino acids to the corresponding zwitterions without either isoelectric precipitation or ion exchange chromatography.

Preliminary evaluation of new polymer matrix for solid-phase extraction of nonylphenol from water samples through Biotage Initiator耐士科技

Molecularly imprinted (MIP) and blank polymers with affinity for nonylphenolwere designed using computational modelling. Chromatographic tests demonstrated higher affinity of imprinted polymers towards the template nonylphenol as compared with blank polymers. The performance of both polymers in solid-phase extraction was however very similar. Both blank and imprinted polymers appeared to be suitable for the removal and preconcentration of nonylphenol from contaminated water samples with 99% efficiency of the recovery. The commercial resins PH(EC) (Biotage) and C18 (Varian) tested in the same conditions used for comparative purposes had recovery rate <84%. The polymer capacity for nonylphenolwas 231mgg?1 for blank and 228mgg?1 for MIP. The synthesised materials can have significance for sample pre-concentration and environmental analysis of this class of compounds.

One-pot SSA-catalyzed b-elimination an efficient and inexpensive through Biotage Initiator耐士科技

Neu5Ac2en1Me per-OAc, the fully protected glycal of sialic acid, is a key intermediate in the discovery of therapeutics and diagnostics, including anti-influenza drugs and proteolysis resistant peptidomimetic foldamers. The synthesis of this sialic acid derivative, however, still relies on standard sugar chemistry that utilizes multi-step methodologies. Herein we report a facile and highly efficient microwave-assisted preparation of Neu5Ac1Me using silica sulfuric acid (SSA) as solid-supported acid catalyst that is one- to two-orders of magnitude faster than standard procedures. We also describe the microwave-assisted and SSA-catalyzed one-pot, rapid, solvent free reaction that combines both peracetylation and b-elimination reactions in one step to generate the glycal from Neu5Ac1Me. We coined the term One-pot SSA-catalyzed Technology for b-Elimination Protocol (OneSTEP) to describe this least laborious, most efficient, and practical preparation to date of Neu5Ac2en1Me per-OAc in terms of yield, time, reagent cost, and waste generation.

Mobility of the Arg-Gly-Asp ligand on the outermost surface of biomaterials suppresses integrin-mediated mechanotransduction and subsequent cell functions by Biotage Initiator耐士科技

Mechanotransduction in the regulation of cellular responses has been previously studied using elastic hydrogels. Because cells interact only with the surface of biomaterials, we are focusing on the molecular mobility at the outermost surface of biomaterials. In this study, surfaces with the mobile Arg-Gly-Asp-Ser(RGDS) peptide have been constructed. Cell culture substrates were coated with ABA-type block copolymers composed of poly(2-methacryloyloxyethyl phosphorylcholine-co-n-butyl methacrylate) segments (A) and a polyrotaxane (PRX) unit with RGDS bound to a-cyclodextrin (B). Adhesion, morphological changes and actin filament formation of human umbilical vein endothelial cells were reduced on the surfaces containing mobile PRX-RGDS in comparison to the immobile RGDS surfaces constructed from random copolymers with RGDS side groups (Prop-andom-RGDS). In the neurite outgrowth assay using rat adrenal pheochromocytoma cells (PC12), only 20% of adherent PC12 cells had neurites on PRX-RGDS surfaces, but more than 50% did on the Random-RGDS surface. The beating colony of dimethyl-sulfoxide-treated mouse embryonic carcinoma cells (P19CL6) were found 10 and 14 days after induction on PRX-RGDS and Random-RGDS surfaces, respectively. After 22 days, the beating colony disappeared on PRX-RGDS surfaces, but many colonies remained on Random-RGDS surfaces. These data suggest that the molecular mobility of the cell-binding ligand on the outermost surface of materials effectively suppresses the actin filament formation and differentiation of these functional cell lines, and may be used as a culture substrate for immature stem cells or progenitor cells.

Microwave-promoted tandem reactions for the synthesis of bicyclic c-lactams by Biotage Initiator耐士科技

A microwave-promoted three-step tandem process for the synthesis of bicyclic c-lactams is developed. In all cases examined this led to significantly faster tandem processes producing the bicyclic c-lactams more cleanly and reproducibly compared to standard thermal conditions.

Microwave-induced by-products in the synthesis of 2-(4-methyl-2-phenylpiperazinyl)pyridine-3-carbonitrile by Biotage Initiator耐士科技

The Letter describes the investigation of an industrial reaction of N-methylphenylpiperazine and chloro nicotinonitrile, under microwave heating. Besides the formation of the expected 2-(4-methyl-2-phe nylpiperazinyl)pyridine-3-carbonitrile (4), extension of the scale leads to unexpected by-products. A specific pathway due to the formation of a reactive ‘ionic alkylating intermediate’ formed in situ under microwave conditions is proposed to explain the results observed.

Microwave-assisted sequential one-pot protocol to benzothiadiazin-3-one-1,1-dioxides via a copper-catalyzed N-arylation strategy by Biotage Initiator耐士科技

A microwave-assisted, sequential, one-pot protocol has been developed for the synthesis of a variety of benzothiadiazin-3-one-1,1-dioxides. This protocol utilizes a copper -catalyzed N-arylation of a-bromobenzenesulfonamides with a number of amines to generate the corresponding 2 aminobenzenesulfonamides, which undergo cyclization to the desired sultams using carbonyl diimidazole (CDI). A range of conditions was evaluated for the key C–N bond formation step with tolerance toward functionalized amines.

Microwave-assisted rapid and straightforward synthesis of 2-aryl-4-quinolones from acylated 20-aminoacetophenones throhgh Biotage Initiator耐士科技

The syntheses of a diverse set of 2-aryl-4-quinolone derivatives were achieved by exposing corresponding acylated 20-aminoacetophenones to microwave irradiation in the presence of NaOH. The microwave accelerated cyclizations were complete within 10–22 min at 120 C giving 57–95% isolated yields.

Microwave-assisted polymerization of higher alkylene oxides through Biotage Initiator耐士科技

Homopolymers and block copolymers of higher epoxides (butene oxide and hexene oxide) are synthesized using 1-alkanols and PEG-MME 1100 as initiators by anionic ring opening polymerization in bulk employing controlled microwave heating in sealed vessels. The selectivity of polymerization of higher epoxides and the effect of different reaction parameters on the formation of side products is discussed. A procedure for the generation of fairly clean homopolymers and multiblock copolymers (giving bottle–brush and cone type of structures) is developed.

Microwave-assisted expeditious and efficient synthesis of cyclopentene ring-fused tetrahydroquinoline derivatives using three-component Povarov reaction by Biotage Initiator 微波合成耐士科技

We report here an efficient and expeditious microwave-assisted synthesis of cyclopentadiene ring-fused tetrahydroquinolines using the three-component Povarov reaction catalyzed by indium (III) chloride. This method has an advantage of shorter reaction time (10–15 min) with high and reproducible yields (up to 90%) and is suitable for parallel library synthesis. The optimization process is reported and the results from the microwave route are compared with those of the conventional synthetic route. In almost all cases, the microwave acceleration consistently provided improved yields favoring the cis-diastereomer.

Microwave-assisted arylation of rac-(E)-3-acetoxy-1,3-diphenylprop-1-ene with arylboronic acids By Biotage Initiator耐士科技

Abstract—The palladium-catalyzed arylation of rac-(E)-3-acetoxy-1,3-diphenylprop-1-ene with arylboronic acids was studied under controlled microwave irradiation conditions. Avariety of different catalysts, bases, and solvents were explored in order to achieve optimum yields in the shortest possible reaction times. The best isolated yields were obtained using Pd2(dba)3$CHCl3/PPh3 as the catalytic system, potassium phosphate monohydrate as the base, and toluene/H2O as a solvent system. Microwave irradiation using 5 mol% of the palladium catalyst for 90 s (max. temp 170 C) generally afforded the cross-coupling products in good to excellent yields.

Microwave assisted synthesis and characterization of end functionalized poly(propylene oxide) as model compounds by Biotage Initiator耐士科技

End functionalized poly(propylene oxide)s with n-alkyl endgroups are synthesized by anionic ring opening polymerization of propylene oxide (PO) in bulk employing controlled microwave heating in sealed vessels. Different alcohols ranging from n-butanol to n-octadecanol are used as initiator and 2–10 propylene oxide units are added on average. A continuous decrease of internal pressure during the sealed vessel experiment reflects the consumption of PO monomer and the completion of the reaction is confirmed by a drop of the internal pressure to zero. The products are characterized by size exclusion chromatography (SEC), liquid chromatography at critical conditions (LCCC) and liquid adsorption chromatography(LAC). SEC with coupled density and refractive index (RI) detection provides information on the chemical composition along the molar mass distribution. LCCC allows a separation of the individual polymer homologous series according to their end groups. In LAC, the alkyl terminated chains elute later than the non-functional chains and can be separated to the baseline according to the number of repeat units.

Metal-assisted synthesis of unsymmetrical magnolol and honokiol analogs and their biological assessment as GABAA receptor ligands by Biotage Initiator耐士科技

We present the synthesis of new derivatives of natural products magnolol (1) and honokiol (2) and their evaluation as allosteric ligands for modulation of GABAA receptor activity. New derivatives were prepared via metal assisted cross-coupling reactions in two consecutive steps. Compounds were tested by means of two-electrode voltage clamp electrophysiology at the a1b2c2 receptor subtype at low GABA concentrations. We have identified several compounds enhancing GABA induced current (IGABA) in the range similar or even higher than the lead structures. At 3 lM, compound 8g enhanced IGABA by factor of 443, compared to 162 and 338 of honokiol and magnolol, respectively. Furthermore, 8g at EC10–20 features a much bigger window of separation between the a1b2c2 and the a1b1c2 subtypes compared to honokiol, and thus improved subtype selectivity.

Indium trichloride catalyzed sp3 C–H bond functionalization through Biotage Initiator耐士科技

Microwave promoted indium trichloride (10 mol %) catalyzed sp3 C–H bond functionalization of 2-alkyl azaarenes 1 or 4 has been observed to construct C–C bond either with but-2-ene-1,4-diones 2 or (E)-3-(2-oxo-2-phenylethylidene)indolin-2-one (6) giving access to 2-((quinolin-2-yl)methyl)butane-1,4-diones 3, 2-((pyridin-2-yl)methyl)butane-1,4-diones 5, or 3-(quinolin-2-yl)propan-2-yl)indolin-2-ones 7 in good yields using 1,4-dioxane as solvent.

Further optimization of novel pyrrole 3-carboxamides for targeting serotonin 5-HT2A, 5-HT2C, and the serotonin transporter as a potential antidepressant through Biotage Initiator微波合成耐士科技

In the continuing search for novel compounds targeting serotonin 5-HT2A, 5-HT2C, and serotonin transporter, new arylpiperazine-containing pyrrole 3-carboxamide derivatives were synthesized and evaluated. Based on the lead reported previously, structural modifications regarding N-(3-(4-(2,3-dichlorophenyl)piperazin-1-yl)propyl)-1,2-dimethyl-5-phenyl-1H-pyrrole-3-carboxamide 5, were accomplished for improvements in not only binding affinity against serotonin receptors and transporter, but also in hERG channel inhibition. Along the line, both the forced swimming tests and spontaneous locomotor activity tests were performed to distinguish between antidepressant activity and false positive results. As potential antidepressant agents, both 2,4-dimethyl-5-phenyl-1H-pyrrole-3-carboxamide and 5-tert-butyl-2-methyl-1H-pyrrole-3-carboxamide derivatives exhibited favorable in vitro and in vivo activities, warranting further investigation around these scaffolds.

First single electron transfer reaction on propargylic chloride in 5-nitroimidazole series through Biotage Initiator耐士科技

We report here the first example of an SRN1 reaction on propargylic chloride in heterocyclic series. The reaction of 4-(3-chloroprop-1-ynyl)-1,2-dimethyl-5-nitro-1H-imidazole with nitronate anions led to both the formation of the C-alkylated product through an SRN1 mechanism and the predominant ethylenic compound resulting from nitrous acid elimination on the C-alkylated product. Interestingly, in contrast to our previous works on SRN1 reactivity, no O-alkylated product was observed.

Domino bicyclization of 2,2-dihydroxyindene-1,3-dione with cyclic enaminones leading to isochromeno[4,3-b]indoles through Biotage Initiator耐士科技

New and practical acid-promoted domino bicyclization between 2,2-dihydroxyindene-1,3-dione and cyclic enaminones has been established for the formation of tetracyclic isochromeno[4,3-b]indoles under microwave heating. The present method simultaneously installs CeN, CeO, and CeC bonds, allowing direct assemble of functionalized isochromeno[4,3-b]indole skeleton with a wide diversity in substituents. The reaction features reliable scalability, flexibility of structural modification, and wide substrate scope as well as operational simplicity, and it can avoid time-consuming and costly syntheses, tedious work-up, and isolation of intermediate.

Cyclocondensation reactions of 5-aminopyrazoles, pyruvic acids and aldehydes. Multicomponent approaches to pyrazolopyridines and related products by Biotage Initiator耐士科技

The reactions of 3-substituted 5-aminopyrazoles with arylidenepyruvic acids and their synthetic precursors, pyruvic acid and aromatic aldehydes, were studied. Several different reaction pathways for these cyclocondensation reactions were established depending on the reaction conditions and building block selection. The formation of pyrazolo[3,4-b]pyridine-6-carboxylic acids as major products and related compounds was discussed from the mechanistic point of view.

Cyclocondensation reactions of 5-aminopyrazoles, pyruvic acids and aldehydes. Multicomponent approaches to pyrazolopyridines and related products by Biotage Initiator耐士科技

The reactions of 3-substituted 5-aminopyrazoles with arylidenepyruvic acids and their synthetic precursors, pyruvic acid and aromatic aldehydes, were studied. Several different reaction pathways for these cyclocondensation reactions were established depending on the reaction conditions and building block selection. The formation of pyrazolo[3,4-b]pyridine-6-carboxylic acids as major products and related compounds was discussed from the mechanistic point of view.

Microwave Reactions Kuniaki

耐士科技作为Biotage中国区总代理，以优质的服务为您提供Biotage全系产品以及相关的技术服务。When the system is processing your experiment, theheating process can be monitored at the Status tab.With the Show Values/Show Graph button, you can toggle between viewing:

采用Biotage Initiator 微波化学合成仪模拟深海热泉的物理化学环境下进行生命起源前氨基酸的合成

为了研究生命起源的深海热泉理论，本文设计了模拟深海热泉环境的体系，即：简单羧-氨水体系和简单羧酸-邻苯二甲酰亚胺体系。本论文采用 BiotageInitiator 微波化学合成仪模拟深海热泉的物理化学环境，在实验过程中压力梯度为 0-18bar，可以模拟到海平面以下 1000 米的水热环境。耐士科技作为Biotage中国区总代理，以最优质的服务给客户提供Biotage全系产品以及相关技术服务。耐士科技作为Biotage中国区总代理，以最优质的服务给客户提供Biotage全系产品以及相关技术服务。

使用Biotage Initiator 微博合成仪进行MnO2纳米线的微波法制

以高锰酸钾为锰源,抗坏血酸为还原剂,在0.5M稀硫酸溶液中通过微波辅助法在160"C温度下加热30而n,得到了形貌规整且尺寸分布均匀的a一MnO:纳棒,其平均直径为50nIn!平均长度超过3娜"研究发现反应的时间和温度对产物的形貌有着重要的影响"通过热重曲线!循环伏安曲线以及恒电流充放电曲线对产物的热学和电学性能进行了表征,结果表明a一MnO:纳米棒具有良好的电化学性能。耐士科技作为Biotage中国区总代理，以最优质的服务给客户提供Biotage全系产品以及相关技术服务。

使用Biotage Initiator微波合成仪帮助进行吡啶吡唑钯类配合物的合成研究

耐士科技作为Biotage中国区总代理，以最优质的服务给客户提供Biotage全系产品以及相关技术服务。本文以吡啶类化合物为原料，设计合成了俩种新型吡啶吡唑类碱水溶性配体，与钯金属原位配位得到具有催化活性的钯配合物，并将其应用于催化Suzuki偶联反应中，得到一系列的联苯类化合物和二苯乙烯类化合物。

使用Biotage Initiator微波合成仪进行稠合吡啶类化合物的合成应用研究

将达米酮或1,3-环己二酮(10 mmo1)、胺(10 mmo1)和乙酸(6 mL)，加入到30 mL Biotage Initiator 2.5微波合成仪专用反应容器中，放入Biotage Initiator 2.5微波合成仪中反应。此混合物先经仪器自动预搅拌10秒，120℃条件下，辐射20-30 min至反应完全，取出冷却后，倒入冰水混合物中，析出黄色沉淀，抽滤得黄色固体，粗产品用无水乙醇重结晶，得到黄色固体产物。耐士科技作为Biotage中国区总代理，以优质的服务为您提供Biotage全系产品以及相关的技术服务。

使用Biotage Initiator微波合成仪进行二氧化锰的合成介绍

耐士科技作为Biotage中国区总代理，以优质的服务为您提供Biotage全系产品以及相关的技术服务。图 1.24 为瑞士 Biotage 公司生产的 Biotage initial 单模微波合成仪。此种合成仪通常采用石英作为反应器的材料，所以其通常适用于液相合成，不适用于纯固相的反应。此为本文所采用的反应仪器。它的主要技术参数为： 微波功率：0-400 W 温度范围：0-250 °C （精度±1 °C） 压力范围：0-2.2 MPa （精度±0.01 MPa） 压力反应罐（包括四种型号）：0.2-0.5 mL，0.5-2 mL，2-5 mL，10-20 mL 搅拌方式：电磁搅拌 (可以根据需求选择搅拌速度)

使用Biotage initiator微波合成仪进行纳米晶体CdS和CdTe的水相合成实验

将前躯体溶液取 4 mL 密封在 5 mL 的石英微波瓶中,放入 Biotage initial 单模微波反应仪中进行微波辐射的水热合成实验。将反应后的产物冷却至室温,开启微波瓶,用丙酮和乙醇的混合溶液对反应产物进行后处理,自然风干后用去离子水复溶,即可得到透明的产物的水溶液。耐士科技作为Biotage中国区总代理，以最优质的服务给客户提供Biotage全系产品以及相关技术服务。

使用Biotage系列产品进行氮杂吲哚及吲哚酮化合物的微波合成以及快速纯化

快速合成含有优势结构的类药分子骨架，有助于构建类药分子筛选化合物库，该部分工作通过多组GBB(Groebke–lackburn–Bienaymé)反应，构建了包含优势结构吡啶并咪唑的衍生三环结构，合成 18 种新结构的化合物，这些化合物在结构上具有潜在的药物活性，在药物虚拟筛选中，这些化合物与靶标酶发生作用从而产生活性的概率更高。耐士科技作为Biotage中国区总代理，以最优质的服务给客户提供Biotage全系产品以及相关技术服务。

使用Biotage Initiator 微波反应进行金属硫化物和氧化物的微波合成

本论文研究了PVP阻止SnS2颗粒团聚的机理。PVP聚合物骨架上的N和O 原子可能首先与锡离子发生杂化,生成一种复杂化合物"聚合物的乙烯骨架的空间效应可能阻止了SnS:颗粒间的团聚"采用微波加热辅助方法,间接地制备了纳米二氧化钟"实验发现通过500摄氏度Zn热处理后,样品的形貌由热处理前的棒状转为球状,而且颗粒的大小达到纳米级"随着温度的增大,晶粒也在长大;温度从300增加到7Oo0C时,纳米晶平均的粒径从5nm变到27nm"温度在500一600℃期间,纳米晶生长迅速。耐士科技作为Biotage中国区总代理，以优质的服务为您提供Biotage全系产品以及相关的技术服务。

使用Biotage Initiator微波合成仪进行酶p300的小分子抑制剂的微波合成

以所筛选的先导化合物结构为基础，通过药物化学和有机合成手段，对先导化合物进行合成、结构优化及新的先导化合物结构的研究，最终到具有高亲和性和选择性的 p300 小分子抑制剂，既可作为研究 p300 生物功能的化学小分子探针，进一步阐明 p300 的生物功能，又能为进一步开发以 HAT 为靶点的药物提供理论基础和实践经验。耐士科技作为Biotage中国区总代理，以最优质的服务给客户提供Biotage全系产品以及相关技术服务。

瑞典Biotage公司最新推出Isolera LS中试级快速制备色谱

耐士科技作为Biotage中国区总代理，以优质的服务为您提供Biotage全系产品以及相关的技术服务。瑞典Biotage公司最新推出Isolera LS中试级快速制备色谱,专为分离纯化大量样品设计,配备750 g和1 500 g硅胶量的SNAP专用分离柱,最多一次可分离超过150 g样品;流速最高达到500 mL /min,只需30 min就可以分离多达几十克样品;秉承了Isole ra系统的所有特点,可紫外双波长自动收集样品,固体和液体上样方式,从TLC方法直接转化为色谱的梯度方法等。该仪器特别适合分离纯化中试样品、合成样品、天然产物等。