新型碱性离子液体催化剂高效催化合成吡喃酮[2,3-d]嘧啶酮和[2,3-d]嘧啶衍生物（英文）

制备了碱性离子液体1,1'-(丁烷-1,4-二基)双(1,4-二氮杂二环[2.2.2]辛烷-1-ium)羟化物,并采用红外光谱、~1H核磁共振谱和pH值分析对其进行了表征.然后将它用于室温研磨条件下高效催化合成吡喃酮[2,3-d]嘧啶酮和[2,3-d]嘧啶.该法步骤简单,反应时间短,产物收率高,无需柱色谱分离,原料易得,且可回收利用.     

新型四氢苯并[4,5]噻吩并[2,3-d]嘧啶酮衍生物的合成及其抗肿瘤活性

以环己酮为原料,利用Gewald反应合成了6个3-烷基-5,6,7,8-四氢苯并[4,5]噻吩并[2,3-d]嘧啶-4-酮衍生物和17个3-亚苄基胺基四氢苯并[4,5]噻吩并[2,3-d]嘧啶-4-酮衍生物,通过1H NMR、13C NMR、IR和MS对所合成的化合物进行了结构表征,并对所合成化合物进行了抗肿瘤活性的筛选.结果表明4个化合物对人鼻咽癌细胞株(KB)和鼻咽鳞癌细胞株(CNE2)两种肿瘤细胞株表现出一定程度的抑制活性.     

水中吡喃并[2,3-d]嘧啶衍生物的洁净合成

以芳醛、丙二腈和2-氨基-4,6-二羟基嘧啶为原料, 以水为溶剂, 在80 ℃以苄基三甲基溴化铵为催化剂一步合成了一系列的吡喃并[2,3-d]嘧啶衍生物, 产物的结构通过IR, 1H NMR和元素分析表征. 该方法反应条件温和、操作简单、收率高. 而且水作为反应溶剂具有廉价、安全、无污染、产物易于分离的优点.     

碱性离子液体催化合成取代萘并吡喃衍生物

离子液体具有强极性、不挥发、化学稳定性好等特点,其极性和亲水/亲脂性可通过改变烷基碳链的长短和阴、阳离子的种类来进行调节,对其结构进行化学修饰,可以得到具有特定功能的离子液体[1-3],因此被誉为绿色溶剂和可设计的溶剂[2]。许多萘并吡喃衍生物都具有重要的生物活性和药     

微波辐射下吡啶[2,3-d]嘧啶衍生物的高效合成

本文以等摩尔的芳醛,巴比妥酸（或1,3-二甲基巴比妥酸）,5-氨基-2-甲基苯[d]噻唑为原料,以醋酸和乙二醇为溶剂,微波辐射下多组分一锅法合成了一系列新的吡啶[2,3-d]嘧啶衍生物。这种方法具有产率高,操作简便,反应时间短等优点。     

吡咯并[2,3-d]嘧啶衍生物的合成方法研究进展

归纳总结了2,4-二氨基吡咯并[2,3-d]嘧啶和2-氨基-4-氧代吡咯并[2,3-d]嘧啶的主要合成方法,并对各方法的优缺点进行了简要评述.参考文献30篇.     

苯并[C]吡喃并[4,3—d]嘧啶类衍生物的合成

苯并［Ｃ］吡喃并［４，３┐ｄ］嘧啶类衍生物的合成王进军周健民陈冰子＊（吉林化工学院精细化工系１３２０２２）（温州医学院基础部３２５０２７）（北京大学生命科学学院１００８７１）３，４－二氢－１Ｈ－苯并［Ｃ］吡喃俗称异色满（ｉｓｏｃｈｒｏｍａｎ），作为某...     

吡唑并[4',3':5,6]吡喃并[2,3-d]嘧啶化合物的合成与生物活性

应用串联氮杂Wittig反应设计合成了一系列新的2-烷氨(芳氧)基-3,8-二苯基-5-芳基-6-甲基-5,8-二氢-4H-吡唑并[4',3':5,6]吡喃并[2,3-d]嘧啶-4(3H)-酮衍生物。通过氢核磁共振谱仪(1H NMR)、傅里叶变换红外光谱仪(FTIR)和元素分析等方法对所合成的化合物进行了结构表征,用X射线单晶衍射确证了化合物2-二正丙基氨基-3,8-二苯基-5-(4-甲基苯基)-6-甲基-5,8-二氢-4H-吡唑并[4',3':5,6]吡喃并[2,3-d]嘧啶-4(3H)-酮(Ⅲi)晶体结构。室内的杀菌和杀虫活性测试结果表明:目标化合物具有一定的杀菌活性,其中部分化合物对黄瓜灰霉菌(Botrytis cinereapers)在50 mg/L剂量下抑制率达到90%以上,显示了优异的杀菌活性;对水稻褐飞虱无明显的杀虫活性,但发现对粘虫具有较高的杀灭效果,大多数抑制率达到90%以上。     

超声辐射下水介质中三组分一锅合成吡喃并[2,3-d]嘧啶衍生物

报道了在超声波辐射下, 水相中无催化剂下通过芳香醛与丙二腈、巴比妥酸的一锅反应, 合成了一系列吡喃并[2,3-d]嘧啶衍生物. 在超声波辐射下, 不仅饱和芳香醛与丙二腈、巴比妥酸的一锅反应在室温下能高收率地进行, 而对于α,β-不饱和醛以及二元醛与丙二腈、巴比妥酸的一锅反应也能在室温下顺利进行, 获得较高的收率. 产物的结构通过IR, 1H NMR和元素分析表征. 该方法具有操作简单和环境友好等优点.     

三乙胺功能化聚乙二醇双子离子液体催化合成吡喃并[2,3-c]吡唑

合成了一种三乙胺功能化聚乙二醇双子离子液体,研究了其作为催化剂,在水相中以芳香醛、丙二腈、乙酰乙酸乙酯、水合肼或苯肼为原料的四组分一锅法反应,制备了16种不同取代基的吡喃并[2,3-c]吡唑化合物,产率为86%~94%.该离子液体稳定性高,可以方便的回收,重复使用5次,活性没有明显的下降.该方法具有反应条件温和,操作简单,产物易分离,对环境友好等优点.     

A novel synthesis of flourinated pyrido [2,3-d] pyrimidine derivatives

Flourinated 4-imino-3,5,7-trisubstituted-pyrido [2,3-d] pyrimidine-2(1H) thiones have been synthesised in good yields by the reaction of 2-amino-3-cyano-4,6- disubstituted-pyridines with various arylisothiocyanates. These new type of products have been characterised by elemental analysis, IR, ¹H and ¹⁹F NMR spectral studies.     

Facile one-pot synthesis of pyrido[2,3-d]pyrimidine derivatives over ZrO2 nanoparticles catalyst

An efficient synthesis of hexahydropyrido[2,3-d]pyrimidinetrione derivatives is achieved via tandem Knoevenagel-Michael addition of aromatic aldehydes,methylcyanoacetate and 4（6）-aminouracil in solvent-free conditions in the presence of 10 mol%of ZrO₂ nanoparticles（ZrO₂ NPs） as a heterogenous catalyst.The procedure is formed in high yields,short reaction time and an environmentally friendly specificity.     

Synthesis of new pyrido[2,3-d]pyrimidine derivatives

The mutual condensation of 4-aminouracil or 2,4-diamino-6-hydroxypyrimidine with bisacetonitrile and aldehydes was used to synthesize 2,4-dioxo-5-R-7-methyl-6-cyano-1,2,3,4,5,8-hexahydropyrido[2,3-d]pyrimidine and 2-amino-4-oxo-5-R-7-methyl-6-cyano-3,4,5,8-tetrahydropyrido[2,3-d]pyrimidine derivatives, which were oxidized with chromic anhydride to the corresponding 2,4-dioxo-5-R-7-inethyl-6-eyano-1,2,3,4-tetrahydropyrido[2,3-d]pyrimidine and 2-amino-4-oxo-5-R-7-methyl-6-cyano-3,4-dihydro[2,3-d]pyrimidines. The IR and UV spectra of the synthesized compounds were recorded.Translated from Khimiya Geterotsiklicheskikh Soedinenii, No. 3, pp. 422–425, March, 1972.     

One-pot synthesis of pyrano[2,3-d]pyrimidinone derivatives catalyzed by L-proline in aqueous media

An efficient protocol has been developed for the synthesis of various pyrano[2,3-d]pyrimidinones from condensation of aromatic aldehydes, malononitrile and barbituric-or thiobarbituric acid in aqueous ethanol using L-proline as a neutral bifunctional catalyst.     

Efficient synthesis of novel furo[2,3-d]pyrimidine derivatives under catalyst-free conditions

A series of furo[2,3-d]pyrimidine derivatives were synthesized via the [3+2] cyclization of pyrimidine-4,6-diol and a variety of nitroolefins at catalyst-free conditions. The reaction is easy to perform simply mixing inexpensive starting materials in water under conventional heating at 90 °C. The reaction proceeds at a fast speed within 1.5–2 h and gives the high biological and pharmacological active substituent furo[2,3-d]pyrimidine derivatives with good to high yields. Mechanism of formation of these furo[2,3-d]pyrimidine derivatives are also proposed.     

Efficient synthesis and In Silico study of some novel pyrido[2,3-d][1,2,4]triazolo[4,3-a]pyrimidine derivatives

A novel series of 1,5-dihydropyrido-triazolo-pyrimidine derivatives were prepared by cyclocondensation of 2-thioxo-pyrido[2,3-d]pyrimidines (prepared from reaction of chalcone with 6-aminothiouracil) with a variety of hydrazonoyl chlorides. Based on spectroscopic evidence and their chemical syntheses, the structures of the newly prepared compounds were elucidated. Designated compounds are forced for molecular docking by using MOE 2014.010 Package software; one of in silico study tools. Synthesized compounds are targeting Human Cyclin-defendant Kinase 2 (CK2) PDB ID (1PXO.Protein data bank) due to its important role in controlling the human cell cycle and also for meiosis.     

Succinimidinium N-sulfonic acid hydrogen sulfate as an efficient ionic liquid catalyst for the synthesis of 5-arylmethylene-pyrimidine-2,4,6-trione and pyrano[2,3-d]pyrimidinone derivatives

Research on Chemical Intermediates - Succinimidinium N-sulfonic acid hydrogen sulfate ([SuSA-H]HSO4) as a new ionic liquid is prepared and characterized using a variety of techniques, including...     

Facile synthesis and antitumor activity of novel 2-trifluoromethylthieno[2,3-d]pyrimidine derivatives

A series of novel 2-trifluoromethylthieno[2,3-d]pyrimidine derivatives were synthesized by a facile three-step procedure that afforded advantages of mild reaction conditions, simple protocol and good yields. The structures of the final compounds were confirmed by 1R, NMR, El-MS, elemental analysis, and X-ray diffraction. Preliminary bioassay results showed that some of the analogs exhibit excellent antitumor activity against MCF-7 and HepG2, especially compounds 3a, 3b, 3e and 3h exhibited higher activity than the positive control gefitinib.