One-pot Preparation of Fluorinated Polyhydrobenzoacridine-1-one Derivatives under Microwave Irradiation and Solvent-free Conditions

A facile and efficient synthesis of fluorine‐containing polyhydrobenzoacridines was accomplished by a three‐component coupling of fluorinated aldehyde, α‐naphthylamine, and 1,3‐cyclohexanedione or dimedone under microwave irradiation and solvent‐free conditions without catalyst. All new compounds were obtained in moderate to good yields and characterized by standard spectroscopic methods.     

Iodine Catalyzed One‐pot Synthesis of 3,4‐Dihydroquinazolin‐4‐ones from Anthranilic Acids,Ortho Esters and Amines under Solvent‐free Conditions

A simple and efficient procedure has been developed for the one‐pot synthesis of 3,4‐dihydroquinazolin‐4‐ones from anthranilic acids, ortho esters and amines using a catalytic amount of iodine under solvent‐free conditions to afford the corresponding products in excellent yields. The direct use of commercially available catalyst, mild and solvent‐free reaction conditions, short reaction time, easy workup and excellent yields are the advantages of the present protocol.     

Uncatalyzed,One-pot Synthesis of 3,3'-(Benzylene)bis(4-hydroxy-2H-chromen-2-one)Derivatives under Thermal Solvent-free Conditions

A series of 3,3′‐(benzylene)bis(4‐hydroxy‐2H‐chromen‐2‐one) derivatives have been synthesized from condensation reactions of 4‐hydroxycoumarin with benzaldehydes under thermal solvent‐free conditions. This environmentally friendly synthesis is uncatalyzed and affords the desired products in excellent yields.     

Oxalic Acid Catalyzed Three Component One Pot Synthesis of 3,4‐Dihydroquinazolin‐4‐ones

An efficient one-pot method for synthesis of an array of 3,4-dihydroquinazolin-4-ones from anthranilicacid, triethyl orthoformate, and anilines using oxalic acid as a catalyst was described. The present protocol offers improvements for the synthesis of 3,4-dihydroquinazolin-4-ones with regard to short reaction time, high yields of products, and simplicity in operation.     

A Simple One-pot Synthesis of Indeno[2,1-f]quinolin-3-one Derivatives under Microwave Irradiation

A series of new indeno[2,1‐f]quinolin‐3(2H)‐one derivatives were synthesized by a reaction of aromatic aldehyde with Meldrum's acid (2,2‐dimethyl‐1,3‐dioxane‐4,6‐dione) and 9H‐fluoren‐2‐amine under microwave irradiation without catalyst in glacial acetic acid. This reaction has notable advantages of short reaction time, high yield and convenient operation.     

Microwave-assisted Synthesis of Pyrazolo[4,3-f]quinolin-7-one Derivatives via Multi-component Reactions

A series of new pyrazolo[4,3‐f]quinolin‐7‐one derivatives were synthesized by multi‐component reactions of equimolar amount of aromatic aldehydes with 2,2‐dimethyl‐1,3‐dioxane‐4,6‐dione and 1H‐indazol‐5‐amine in ethylene glycol without catalyst under microwave irradiation. This one‐pot protocol has the advantage of good yields, simple workup procedure and shorter reaction time.     

LiBr as an Efficient Catalyst for One-pot Synthesis of Hantzsch 1,4-Dihydropyridines under Mild Conditions

A simple, inexpensive and efficient one‐pot synthesis of 1,4‐dihydropyridines has been accomplished via lithium bromide‐catalyzed Hantzsch three‐component condensation reaction of an aldehyde, α,β‐ketoester and ammonium acetate in acetonitrile at room temperature in good to excellent yields. The present protocol is applicable to wide range of substrates including aliphatic, aromatic and heterocyclic aldehydes affording 1,4‐dihydropyridines.     

2-氨基-3-氰基-4-芳基-4H-苯并[h]苯并吡喃的一步合成

结构;2-氨基-3-氰基-4-芳基-4H-苯并[h]苯并吡喃的一步合成     

Tandem One‐pot Synthesis of Polysubstituted 1,3‐Thiazine Derivatives

A tandem one‐pot synthesis of polysubstituted 1,3‐thiazines has been developed by reacting with cyanoacetamide and isothiocyanate derivatives to give rise to 2‐cyano‐3‐mercaptoacrylamides, which are trapped in situ by various aldehydes or diversely substituted ketones through intermolecular cyclization, providing polysubstituted 1,3‐thiazine derivatives in short reaction times with good to excellent yields. The salient features of this novel protocol are operational simplicity, accessing the desired products from the readily available starting materials and easy of product isolation and may find wide spread applications in medicinal chemistry.     

One‐pot synthesis of 3,4‐dihydropyridin‐2‐ones via tandem reaction of Blaise reaction intermediate and acrylic ester

An efficient method for the synthesis 3,4‐dihydropyridin‐2‐ones has been developed via tandem one‐pot Michael‐type addition and cyclization of the Blaise reaction intermediate and acrylic ester. A series of readily available nitriles, bromoacetic esters and acrylic esters have been employed to examine the scope of substrates for this method. Copyright © 2015 John Wiley & Sons, Ltd.     

A Novel Method for One‐pot Synthesis of Furo[3,2‐c]coumarin Derivatives from 4‐Hydroxycoumarin and Arylglyoxal under Microwave Irradiation

A novel one‐pot synthesis of furo[3,2‐c]coumarins has been developed from readily available starting materials 4‐hydroxycoumarin and arylglyoxal. This method is simple, rapid and good yielding.     

A Novel One‐pot Synthesis of Biaryl Derivatives by Sequential Strategies via Suzuki Coupling/Knoevenagel Condensation in Aqueous Medium at Room Temperature

A novel one‐pot synthesis of biaryl derivatives has been developed starting from bromobenzaldehyde and phenylboronic acid in the presence of activated methylene compounds via sequential Suzuki coupling/Knoevenagel condensation in aqueous isopropanol medium at room temperature. Significantly, this strategy afforded a straightforward and efficient approach to construct original biaryls in which a new carbon double bond bound to activated moieties such as nitrile, ester and amide is formed from three simple substrates in a one‐pot procedure. Moreover, a wide scope of substrates could effectively participate in the process affording the target products in moderate to excellent yields.     

新型氮杂异香豆素化合物的合成

以4-氯烟酸和芳基乙腈为原料,经取代和环合反应合成了3个新型的氮杂异香豆素化合物（3a~3c）,收率32.1%~89.0%,其结构经¹H NMR, IR, ESI-MS和元素分析表征。用X-单晶衍射研究了3a的亚甲基衍生物（4a）的晶体结构。4a(CCDC: 935 919)属三斜晶系,空间群P ī, 晶胞参数a=6.881(2) , b=9.768(2) , c=11.809(2) , β=104.125(10)°, V=732.1³, Dc=1.331 mg·cm^-3 , Z=2, F(000)=308, μ=0.090 mm^-1。并对环合反应机理进行了研究。     

Reactivity-based One-pot Synthesis of Immunosuppressive Glycolipids from the Caribbean Sponge Plakortis simplex

The first synthesis of three natural glycolipid simplexides 1a – 1c , which were isolated from the marine sponge Plakortis simplex and claimed to inhibit T cell proliferation, has been concisely accomplished by a reactivity‐based one‐pot synthetic strategy under the use of p‐toluenethioglycoside (STol) donors.     

One-pot Synthesis of 1,8-Dioxo-decahydroacridine Derivatives in Aqueous Media

A new and efficient method for the synthesis of 1,8‐dioxo‐9‐aryl‐decahydroacridine derivatives was developed via a one‐pot three component reaction of dimedone, aromatic aldehydes and ammonium acetate in the presence of ammonium chloride, or Zn(OAc)₂·2H₂O or L‐proline separately in water in the short period of time and high yields.     

超声法合成3,4-二氢嘧啶-2(1H)-酮衍生物

以取代芳醛（1a~1h）,乙酰乙酸乙酯(2)和脲(3)为原料,MMT/CuCl₂为催化剂,乙醇为溶剂,在超声条件下经Beginelli反应合成了8个3,4-二氢嘧啶-2(1H)-酮衍生物（4a~4h）,其结构经¹H NMR和IR确证。以4a为例,分别采用单因素法和正交实验法研究了催化剂、溶剂、反应温度、超声时间和物料比r［n(1a): n(2) :n(3)］对4a产率的影响。结果表明：在最优反应条件(1a 2.4 mol, r=1.2 : 1.0 : 1.0, MMT/CuCl₂20 mol%, EtOH 1 mL,于90 ℃超声15 min)下,4a产率88.4%。 MMT/CuCl₂循环使用3次,产率基本不变。     

Biginelli 3,4-二氢嘧啶-2-酮衍生物的合成研究新进展

1893年, 意大利化学家Biginelli首次利用芳香醛、乙酰乙酸乙酯和尿素三组分“一锅煮法”合成了3,4-二氢嘧啶-2(1H)-酮. 此类化合物具有良好的生物活性和反应活性, 对近几年来有关Biginelli 3,4-二氢嘧啶-2(1H)-酮的衍生化反应、Biginelli不对称合成和Biginelli反应在天然产物合成中的应用研究进行了综述.     

Synthesis and Vasodilatory Activities of New Pyrazolo[3,4—d] pyrimidin—4—one Derivatives

A series of pyrazole[3,4-d] pyrimidin-4-one derivatives were synthesized and tested for vasodilatory activities. All of them were new compounds and their structures were confirmed by IR,^1H NMR,MS and elemental analysis.     

对硝基甲苯合成3,4-二甲基苯胺的研究

以对硝基甲苯为原料,经胺甲基化、水解、还原3步反应合成了目标化合物。通过单因素实验,分析每一步反应的关键影响因素,初步得到适宜的合成条件。最终产物的结构经核磁氢谱、质谱、元素分析进行确证,纯度经气相色谱分析。3,4-二甲基苯胺的总收率56.6%,纯度大于98.5%。该合成路线原料易得,成本较低,操作简单。     

Application of Heteropolyacids as Heterogeneous and Recyclable Catalysts for One-Pot Synthesis of 3-Cyanopyridine Derivatives

A simple, clean and environmentally benign route to the synthesis of 3-cyanopyridines is described via a one-pot multi-component reaction of 3,4-dimethoxyacetophenone, malonitrile or ethylcyanoacetate, aldehyde and ammonium acetate using heteropolyacids as heterogeneous and recyclable catalysts in very good yields.