A New Solution—phase Parallel Synthesis of 2—Alkyamino—3—aryl—5—phenylmethylene—3,5—dihydro—4H—imidazol—4—ones

Thirteen new 2-alkylaminoimidazolones(4) wre rapidly synthesized by a new solution-phase parallel synthetic method,which includes aza-Wittig reaction of iminophosphorane(1) with aromatic isocyanate to give carbodi-imide(2) and subsequent reaction of 2 with various aliphatic primary amine in a parallel fashion.The products were confirmed by ^1H NMR,MS,IR and X-ray crystallographic analysis.The unusual selectivity of the cyclization was probably due to the deometry of the guanidine intermediate.     

Synthesis and Biological Activities of 3—（2—Furyl）—4—aryl—1,2,4—triazole—5—thiones

A series of novel compounds 3-(2-furyl)-4-aryl-1,2,4-triazole-5-thiones have been synthesized.All the compounds were characterized by spectral data and elemental analysis. The preliminary biological test showed that some of them exhibited excellent plant-growth regulative activities.     

Synthesis of 5—Aryl—1,2—dihydro—1—pyrrolizinones

In order to search for new potent anti-inflammatory and analgesic agents in pyrrolizinones,the title compounds were designed and synthesized.A series of the compounds were prepared with two different synthetic schemes.Some of the compounds showed remarkable anti-inflammatory and/or analgesic activities on mice.     

Dramatic Solvent Effect in the Reduction of 2,3—Allenoic Acid Esters.A Simple Synthesis of 2,3—Allenols from 2,3—Allenoates

2，3－Allenols were prepared conveniently from the reduction reaction of 2,3-allenoates with DIBAL-H(Diisobutylaluminum hydride) in toluene.A dramatic solvent effect was observed for this reaction.     

One-pot Synthesis of 3-Aryl-1,5-bis（2-hydroxyaryl）pentane-1,5-diones

A simple method for the synthesis of 3-aryl-1,5-bis(2-hydroxyaryl)pentane-1,5-diones is developed by one-potreaction involving 2-hydroxyacetophenone and arylaldehyde in aqueous potassium hydroxide.     

Synthesis of 4—Aryl—3,4—dihydropyrimidinones Using Microwaveassisted Solventless Biginelli Reaction

Ｉｎｔｒｏｄｕｃｔｉｏｎ4 Ａｒｙｌ 3,4 ｄｉｈｙｄｒｏｐｙｒｉｍｉｄｉｎｏｎｅｓ (4)ａｓａｃｏｒｅｗｅｒｅｏｂｓｅｒｖｅｄｉｎｓｏｍｅｂｉｏｌｏｇｉｃａｌｌｙｉｍｐｏｒｔａｎｔｃｏｍｐｏｕｎｄｓ .1Ｍｏｒｅｒｅｃｅｎｔｌｙ ,ｄｉｈｙｄｒｏｐｙｒｉｍｉｄｉｎｏｎｅｓａｒｅｓｈｏｗｎｔｏｂｅａｕｓｅｆｕｌｔｏｏｌｆｏｒｓｔｕｄｙｉｎｇｄｙｎａｍｉｃｃｅｌｌｕｌａｒｐｒｏｃｅｓｓａｎｄｃａｎｂｅｃｏｎｓｉｄｅｒｅｄａｓａｎｅｗｌｅａｄｆｏｒｔｈｅｄｅｖｅｌｏｐｍｅｎｔｏｆａｎｔｉ ｃａｎｃｅｒｄｒｕｇ…     

Synthesis of 3,7—Disubstituted 1,4—Benzodiazepin—2—one

A series of 3-methoxycarbonylpropoxy-7-(imidazol-4-ylpropinamide)-1,3-dihydrogen-1-methyl-5-phenyl-2H-1,4-benzodiazepin-2-ones,as farnesyltransferase(Ftase) inhibitors,were synthesized. The preparation of the key intermediate,7-amino-3-methoxycabonylpropoxy-1-methyl-5-phenyl-2H-1,4-benzodiazepin-2-one,was improved.     

Synthesis of （1H）—3,4—Dithydropyrrolo[2,1—c][1,4]oxazin—1—one Derivatives

In search of new anti-inflammatory and analgesic agents,(1H)-3,4-dihydro-pyrrolo [2,1-c][1,4]oxazin-1-one(3) and its acyl derivatives were designed and prepared .Compound 3 was prepared by treatment of methyl 1-(2-bromoethyl) pyrrole-2-carboxylate with silver oxide and its derivatives were obtained by Friedel-Carftes reaction.Nine of 6-acyl derivatives of compound 3 were prepared.     

Palladium Catalyzed Synthesis of Fluorine-containing 3-Biaryl-1-ferrocenyl-2-propene-1-one

In the last two decades, molecular-based second-order nonlinear optical (NLO) chromo-phores1, have attracted much interest because of their potential applications in emerging 2opto-electronic technologies. These efforts have mainly focused on organic systems.More recently, organometallic molecules have been investigated as well. In comparisonto common organic molecules, they offer a large variety of novel structures3, . The 4possibility of high environmental stability, and divers…     

A Convenient Palladium-Catalyzed Carbonylative Synthesis of (E)-3-Benzylidenechroman-4-ones

A convenient palladium-catalyzed carbonylation reaction for the efficient synthesis of (E)-3-benzylidenechroman-4-ones has been developed. Using TFBen as a solid CO source, a range of substituted (E)-3-benzylidenechroman-4-ones were prepared in moderate to good yields with 2-iodophenols and allyl chlorides as the substrates. Additionally, substituted quinolin-4(1H)-ones can also be obtained with 2-iodoaniline as the starting material.     

Facile construction of symmetric biaryls using (BeDABCO)2Pd2Cl6 as an efficient and highly active catalyst under microwave irradiation

An efficient catalytic system using (BeDABCO)₂Pd₂Cl₆ (BeDABCO, benzyl‐1,4‐diazabicyclo[2.2.2]octane) was developed for the homo‐coupling reaction of various aryl halides. Due to the combination of ionic homogeneous metal catalyst and microwave irradiation, symmetric biaryls were produced in excellent yields and short reaction times in N‐methyl‐2‐pyrrolidone at 120 °C. BeDABCO as an efficient ligand and also a quaternary ammonium salt had an efficient stabilizing effect on the Pd(0) species in this coupling reaction. Copyright © 2015 John Wiley & Sons, Ltd.     

羧基亚胺配体的合成及其促进Suzuki偶联反应的研究

合成了4种羧基亚胺配体并将其用于促进Suzuki偶联反应。通过考察配体结构、溶剂极性、碱强度和温度等因素对反应产率的影响,确定了羧基亚胺配体参与的钯催化Suzuki偶联反应的最佳条件为:催化剂的量为0.001(mol)%的Pd Cl2和0.002(mol)%的配体,以碳酸钾作碱,4m L乙醇水溶液(1∶1,体积比)作溶剂,反应温度为60℃,在空气条件下反应。结果表明,羧基亚胺配体能够有效促进Suzuki偶联反应;在合成的配体L1~L4中,具有适当的位阻和给电子基团的L2的催化活性最高,能够高效催化合成一系列联芳类化合物。     

含二茂铁的双取代哒嗪的合成和介晶性

合成了8个未见报道的中心桥连基为哒嗪环、酯基、CHN基,含有二茂铁、三个苯环、不同末端链长度的双取代哒嗪化合物,并通过示差扫描量热仪(DSC)对其介晶性进行了表征.研究表明,末端链长度对相变温度和清亮点温度均有影响,但对相变温度范围影响较小.     

Novel Synthesis and Crystal Structure of 2-(4-Methylphenyl)-3-ferrocenyl-4,4-dicyanpyrrolizidine

A novel ferroenyl pyrrolizidine derivative containing cyano groups, 2-(4-methylphenyl)-3-ferrocenyl-4,4-dicyanpyrrolizidine (C26H25FeN3 , Mr=435.34), was synthesized in moderate yields via a facile 1.3-dipolar cycloaddition in refluxing toluene and its crystal structure was determined by single-crystal X-ray diffraction. It crystallizes in monoclinic, space group P21/c with a=10.3792(10), b=11.4485(11), c=19.1243(15), β=109.496(4)°, V=2142.2(3)3, Dc=1.350 g/cm3, μ(MoKα)=0.721 mm-1 , Z=4, T=113(2)K, F(000)=912, the final R=0.0586 and wR=0.1664.     

壳聚糖席夫碱钯催化碘代苯与丙烯酸乙酯反应

以水杨醛与壳聚糖反应制得的壳聚糖席夫碱配体再与PdCl2反应制得了壳聚糖席夫碱钯催化剂。研究了该催化剂对碘代苯(PhI)与丙烯酸乙酯(EA)偶联生成反式肉桂酸乙酯反应的催化性能。考察了原料比、缚酸剂种类及其用量、反应温度、溶剂、催化剂用量、反应时间等因素对该反应的影响,确定了该催化反应的最佳反应条件。该催化剂经过滤分离、溶剂洗涤,循环使用4次仍有较高的催化活性。     

Synthesis of 1,5-naphthylethynyl nanostructure networks with extended π-conjugation. Effective heterocoupling catalyzed by palladium under a compatible CO2 atmosphere

The synthesis of a new extended π-conjugated 5-N,N-dimethylaminonaphthyl family was undertaken by palladium-catalyzed cross-coupling reaction between a protected 5-iodonaphthylethynyl and 1-ethynyl-5-(N,N-dimethylamino)naphthalene. Under an argon atmosphere, only the homocoupling product 1,4-(N,N-dimethylamino)naphthyl-1,3-butadiyne was isolated, in excellent yield. However, under a compatible and pure carbon dioxide atmosphere, the cross-coupling product was obtained in excellent yield.     

Synthesis, structure and biological activity of 1-(1-methoxy-1-ferrocenyl-3-arylpropan-2-yl)-1H-1,2,4-triazole derivatives

A total of eleven new 1-(1-methoxy-1-ferrocenyl-3-arylpropan-2-yl)-1H-1,2,4-triazole derivatives have been synthesized from acetylferrocene. The structures of the title compounds have been determined by elemental analysis, ¹H-NMR and single crystal X-ray diffraction analysis. Bioassay showed that some of the title compounds had high plant-growth regulatory activity. __________ Translated from Chinese Journal of Organic Chemistry, 2005, 25(8) (in Chinese)     

钯-二茂铁配合物催化的suzuki-miyaura偶联反应

suzuki-miyaura偶联反应;二茂铁;溴苯;苯硼酸;钯