3,4-二胺-1H-吡唑并[5,4-d]嘧啶的固相合成

用固相合成技术合成了吡唑并[5,4-d]嘧啶的一类衍生物8.以Merrifield树脂为原料,与化合物3反应得到树脂4.4经过还原胺化、取代、分子内亲核加成反应得到树脂7,再由三氟醋酸断裂得到化合物3,4-二胺-1H-吡唑并[5,4-d]嘧啶.     

吡唑啉衍生物的合成及应用研究进展

吡唑啉衍生物是一类应用广泛的重要五元含氮杂环化合物,在医药、农药等生物领域和其他非生物领域都具有非常重要的应用价值与广阔的应用前景.作者简单概述了吡唑啉衍生物的合成及其应用方面的研究进展.     

吡唑类化合物的合成研究进展

吡唑类化合物是一类重要的药物合成中间体,在抗肿瘤、抗病毒、抗抑郁等领域发挥着重要作用。本文综述了吡唑类衍生物的合成方法,包括1,3-亲电化合物与肼类的环化、1,3-偶极体系的环加成等。     

3-苄硫基-5-重氮基-4-乙氧羰基吡唑的合成、晶体结构的确定及反应活性的研究

吡唑类衍生物是一类具有很好生物活性的化合物,具有很高除草或杀虫活性的吡唑类化合物文献中已有大量的报导^[1]。因此研究其合成方法显得很重要。我们最初希望通过5-氨基-3-苄硫基-4-乙氧羰基吡唑经重氮化反应去氨基制备3-苄硫基-4-乙氧羰基吡唑,然后继续衍生化合成系列吡唑类化合物。     

铜催化环酮亚胺与β,γ-不饱和N-酰基吡唑不对称Mannich-Type反应

手性苯并环状磺酰胺是一类重要的生物活性化合物和功能性有机分子,发展其高效的不对称催化合成方法一直备受关注.铜催化环状N-磺酰亚胺与β,γ-不饱和N-酰基吡唑的不对称Mannich-type反应是一类新合成策略.在温和反应条件下,该方法以良好的产率,优异的选择性(区域选择性(γ/α>20/1)、非对映选择性(dr>20/1)、对映选择性(upto93%ee)得到γ-加成产物手性苯并五元环状磺酰胺,且底物范围较广,官能团兼容性较好,为结构多样的手性苯并环状磺酰胺及其衍生物合成提供新的合成途径.     

α-二乙硫基亚甲基酰胺与肼[3+2]合成多取代吡唑的研究

吡唑类化合物是一类具有独特生物活性以及药理活性的杂环类化合物,被广泛应用在药剂及农药产品的合成.本论文在95％乙醇溶剂中,K2CO3为碱,通过α-二乙硫基亚甲基酰胺和肼[3+2]环合反应,一步高效合成了一系列多取代吡唑类化合物,化合物结构经1H NMR,13C NMR和HR-MS(ESI)进行了表征,并对该合成反应机理...     

酰基吡唑啉酮化合物的计算、合成和抑菌活性

利用Sybyl 6.3软件包中的分子力学程序对2个4-酰基-2-吡唑啉-5-酮类化合物分子进行了系统研究,得到了它们的最低能量构象,发现它们具有适宜的配位环境,可能是一类新型的三齿配体。 合成和表征了1-苯基-3-甲基-4-(邻-甲酰基苯甲酸)-2-吡唑啉-5-酮 和1-苯基-3-甲基-4-(顺-乙酰基丁烯酸)-2-吡唑啉-5-酮化合物。 抑菌活性测定结果表明它们对革兰氏阳性和阴性菌均有较好的抑制作用,为进一步研究其配合物的生理活性提供了参考依据。     

四二茂铁甲酰基四氮杂对环蕃的合成

在设计和合成新的分子受体中环蕃担任了重要角色[1,2],可用于对映异构体和非对映异构体的分子识别[3,4],四氮杂对环蕃是人工模拟酶研究中发现的一类新化合物,也是主-客体化学中可以充当主体的一类重要化合物.对这一类化合物的合成及修饰,可能产生理想的酶模型用于加快反应速率,或选择性地控制反应.     

新型吡唑并[1,5-a]嘧啶-氮芥衍生物的设计、合成及抗肿瘤活性研究

吡唑并嘧啶是一类具有广泛生物活性的杂环结构母体,同时,氮芥类药物被广泛应用于临床治疗癌症.本文基于药物设计的拼合原理,以简单易得的原料制备了取代吡唑并[1,5-a]嘧啶中间体,通过将其与苯胺氮芥组分进行拼接,合成了一系列新型吡唑并[1,5-a]嘧啶-氮芥化合物,并评估了目标化合物对五种不同肿瘤细胞(HepG2、SH-S...     

羰基α-位胺化反应研究进展

α-氨基羰基衍生物是一类重要分子骨架,存在于许多药物分子和天然产物分子中;同时,也是一类重要的有机合成中间体,用于合成许多重要的有机化合物分子.发展简单、高效的方法合成结构多样性的α-氨基羰基衍生物具有重要的研究意义.总结了近几十年来羰基α-位碳氢键的直接胺化反应,根据反应所经历的不同活化模式,对这类反应进行了分类总结,主要分为亲电胺化、氧化胺化、卤化物介导的胺化和电化学胺化四类反应.     

Synthesis of 1,3-diketones from 3-(4-R-phenyl)propionic acids

Self-acylation of 3-(4-R-phenyl)propionic acids (R = H, Br, 1-adamantyl) in trifluoroacetic anhydride catalyzed by trifluoromethanesulfonic acid provides a simple and efficient synthesis of 1,3-diketones. Indan-1-ones formed in the first step undergo acylation to give the corresponding 2-(3-phenyl-1-oxopropyl) indan-1-ones as the major products. One-pot synthesis of polysubstituted pyrazoles directly from 3-(4-R-phenyl)propionic acids is described.     

Visible-light promoted one-pot synthesis of pyrazoles from alkynes and hydrazines

A visible-light promoted cascade of Glaser coupling/annulation has been developed for one-pot synthesis of polysubstituted pyrazoles from alkynes and hydrazines. The method features mild reaction conditions, readily availible starting materials and green oxidant (O₂). It works for a wide range of substituted phenyl acetylene and hyrazines with good functional group tolerance and efficiency. Mechanistic pathways including photochemical irridiation, intramolecular hydrogen-atom-abstraction (HAT) and enamine-to-imine tautomerization was proposed for the transformation.     

A facile approach to polysubstituted pyrazoles from hydrazonyl chlorides and vinyl azides

A novel and facile approach to polysubstituted pyrazoles from readily synthesized hydrazonyl chlorides and vinyl azides was developed. The reaction was regiospecific and proceeded under mild conditions in the presence of base.     

Nitriles in organic synthesis: The reaction of trichloroacetonitrile with active methylene reagents

The reaction of trichloroacetonitrile with active methylene reagents such as acetylacetone, benzoylacetone, cyanoacetamide and cyanoacethydrazide is reported. A new simple route for the synthesis of polysubstituted phenols, pyrazoles and pyrroles is also described.

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Nitrile bei organischen Synthesen: Die Reaktion von Trichloracetonitril mit aktiven Methylen-Reagentien

Zusammenfassung Es wird über die Reaktionen von Trichloracetonitril mit aktiven Methylen-Reagentien wie Acetylaceton, Benzoylaceton, Cyanacetamid und Cyanacethydrazid berichtet. Ein neuer einfacher Weg für die Synthese polysubstituierter Phenole, Pyrazole und Pyrrole wird beschrieben.

     

Substituted Pyrazoles and Their Heteroannulated Analogs—Recent Syntheses and Biological Activities

Pyrazoles are considered privileged scaffolds in medicinal chemistry. Previous reviews have discussed the importance of pyrazoles and their biological activities; however, few have dealt with the chemistry and the biology of heteroannulated derivatives. Therefore, we focused our attention on recent topics, up until 2020, for the synthesis of pyrazoles, their heteroannulated derivatives, and their applications as biologically active moieties. Moreover, we focused on traditional procedures used in the synthesis of pyrazoles.     

Synthesis of Pyrazole Derivatives Possessing Anticancer Activity: Current Status

Pyrazole is a versatile lead compound to design potent bioactive molecules for drug discovery and development, particularly in cancer therapy. The aim of this review is to present the most recent deeds in the field of synthetic route made for functionalized pyrazole derivatives active against cell proliferation disease. The review article covers the synthesis of 1H-pyrazole, synthesis of N-substituted pyrazoles, synthesis of pyrazolopyrazoles, and synthesis of pyrazoles fused with a naturally occurring moiety. Some of these reported compounds have passed the preclinical or initial-phase clinical trials for their anticancer activity.     

Synthesis of Functionalized 2-(2-Pyrrolyl)pyrazolo[1,5-a]pyrimidines

Reactions of 5-amino-3-(2-pyrrolyl)pyrazoles with -dicarbonyl compounds (acetylacetone and ethyl acetoacetate) lead to formation of up to 90% of polysubstituted pyrazolo[1,5-a]pyrimidines.     

Synthesis and transformations of methyl (E)-2-(acetylamino)-3-cyanoprop-2-enoate und methyl (E)-2-(benzoylamino)-3-cyanoprop-2-enoate,versatile reagents for the preparation of polyfunctional heterocyclic systems

Methyl (E)-2-(acetylamino)-3-cyanoprop-2-enoate ( 2a ), and its 2-benzoyl analog 2b ere prepared from the corresponding methyl (Z)-2-(acylamino)-3-(dimethylamino)propenoates 1 Multifunctional compounds 2 are versatile synthons for preparation of polysubstituted heterocyclic systems such as pyrroles 4 , pyrimidines 5 and 6 , pyridazines 7 , pyrazoles 8 , 9 , and 11 , and isoxazoles 10 .     

叶绿素-a衍生物的化学反应和多取代卟吩(啉)合成的研究进展

天然产物叶绿素-a衍生物所具有的特殊理化性质以及连带多种活性取代基团的非对称性骨架结构, 决定其化学反应的活泼性和实际应用的广泛性. 基于以叶绿素-a及其衍生物为研究对象的化学反应和结构修饰, 综述了近期多取代卟吩(啉)合成的研究进展.     

Synthesis of new polysubstituted (pyrazoles, pyrimidines and quinolines) five and six-membered heterocycles: reaction of α,α-dioxoketene dithioacetals with nucleophiles

A novel synthesis of polysubstituted pyrazoles 3a-d, pyrimidines 4a-f and quinolines 5a-c via the reaction of α,α-oxoketene dithioacetals 2a-c with hydrazine hydrate, malonohydrazide, urea, thiourea and aniline is reported and the synthetic potential of the method is demonstrated. The structure of the new compounds was established upon their elemental analysis, IR, ¹H NMR and ¹³C NMR.