4—甲基—7—巯基—2（1H）—喹啉酮的合成

以间氨基苯硫酚为起始原料,与乙酰乙酸乙酯一步环合得目标产物4－甲基－7－巯基－2（1H)-喹啉酮（4）,收率：22％;以间苯二胺为起努原料,经乙酰乙酸乙酯环合,重氮化,二硫化合物的形成及盐酸锌和粉还原获得目标产物4,收率：59％。     

4，4‘—[1,n—亚烷基双[（E）—2—（4—氧基苯）乙烯基]]双吡啶的光化学性质

通过E-[4-[2-(4-羟基苯基）乙烯基]吡啶与1，n－二溴烷烃亲核取代反应合成了4，4‘-[1,n－亚烷基双[（E）－2－（4－氧基苯）乙烯基]]双吡啶[n=2(Ia),3(Ib),4(Ic),6(Id)]。用元素分析、红外、紫外和质子核磁共振谱鉴定了Ia-Id的结构。将Ia-Id的稀溶液用中压汞灯和低压汞灯交替照射，发现其分子内光环加成反应的存在，并且随着亚烷基碳链的延长，反应速度加快。研究还发现锌离子可以与吡啶环上氮原子发生螯合作用使分子内光环加成反应加快。本文化合物荧光很弱，在较高浓度下有较强分子间激基缔合物荧光。     

1,4-二氢-2,6-二甲基-4-(3-硝基苯基)-3,5-吡啶二羧酸二(2-甲氧基乙基)酯的合成

对1，4－二氢吡啶类钙拮抗剂西尼地平进行了结构修饰。以双乙烯酮和乙二醇单甲醚为原料，经酯化、缩合、氨化和Hantzsch环化等反应合成了1，4－二氢－2，6二甲基－4－（3－硝基苯基）－3，5－吡啶二羟酸二（2－甲氧基乙基）酯，总收率71％。目标产物结构经^1H NMR和MS确证。     

2,2'－联吡啶桥连的双－4,4'-联吡啶哑铃型化合物的合成

二甘醇2与对甲苯磺酰氯在CH_2Cl_2中，0 ℃～r.t.及Et_3N存在下反应得2－ （羟乙氧基）乙醇对甲苯磺酸酯（3），收率88％。化合物3与对叔丁基苯甲酰氯在 CH_2Cl_2中0～5 ℃及吡啶存在下反应得2－（对叔丁基苯甲酰氧基乙氧基）乙醇对 甲苯磺酸酯（4），收率96％。4与对羟苯甲醇在乙腈中及CsF/K_2CO_3存在下70 ℃ 反应得2－（对叔丁基苯甲酰氧基乙氧基）乙氧苄醇（5），收率98％。5与NBS及 PPh_3在THF中，室温下反应得化合物2－（对 丁基苯甲酰氧基乙氧基）乙氧苄溴 （6），收率95％。6与4,4'－联吡啶在乙腈中，60 ℃反应1h得N－[2－（对叔丁基 苯甲酰氧基乙氧基）乙氧苄基]－4,4'－联吡啶六氟磷酸盐（7），收率85％。7与 α,α－二（溴甲基）－2,2'－联吡啶在乙腈中，油浴60 ℃反应36h，得到标题化 合物，产率为45％。     

4—乙烯基吡啶—镍（钴）及丙烯酰胺—镍（钴）的制备、结构、聚合及聚合物

制备了4－乙烯基吡啶－镍（钴）和丙烯酰胺－镍（钴）络合物并研究了它们的结构。在自由基引发剂的作用下，4－乙烯基吡啶－镍可进行溶液聚合，也可与苯乙烯共聚合，测定了单体的竞聚率。所得的聚（4－乙烯基吡啶－镍）及聚（4－乙烯基吡啶－钴）以NαBH4还原后可作为一些有机化合物的加氢催化剂。由IR及XPS分析说明在丙烯酰胺－镍 合物中，与镍离子发生了络合作用的是碳基上的氧原子。     

聚乙烯吡啶(PVP)催化合成O-酰化乳酸酯的研究

本文利用聚乙烯吡啶（ｐｏｌｙｖｉｎｙｌ ｐｙｒｉｄｉｎｅ）为催化剂，对乳酸酯进行Ｏ－酰化反应，对影响反应的诸因素进行了讨论，产物的收率为７０－８０％。     

E—1、Z—2（1—咪唑基）—O—（α—甲基对卤苄基）2′，4′—二氯苯乙酮肟硝酸盐的合成与结构表征

首先以2,4－二氯氯代苯乙酮、咪唑、羟胺和对卤苯乙酮为原料,分别合成E－、Z－2－1（1－咪唑基）－2′,4－′二氯苯乙酮肟（IE、IZ）和对卤α－氯乙苯（ⅡA和ⅡB）,ⅠE和ⅠZ分别与ⅡA和ⅡB反应,生成E－、Z－2－1（1－咪唑基）－O－（α－甲基对卤苄基）－2′,4′－二氯苯乙酮肟硝酸盐四个新化合物,产率炒52．0％－60．0％,并经元素分析、IR和^1HNMR进行了表征。     

含三唑啉硫酮槟榔碱衍生物合成和生物活性

烟酸经酯化、肼解、与取代芳酸异硫氰酸酯缩合成1－（3－吡啶甲酰基）－4－芳基氨基硫脲（2），2经环合成生成2－（3－吡啶）－4－芳基－1，3，4－三唑啉－5－酮（3），接着用碘甲烷对吡啶环季铵化得相应的季铵盐4，4用硼氢化钠还原可得目标物2－（1－甲基－1，2，5，6－四氢吡啶－3－4）－4－芳基－1，2，4－三唑啉－5－硫酮（5），对所合成的目标化合物进行了舒张血管活性实验。     

α—（α′—甲基—卤代苄氧基）—β—（1—咪唑基）—2，4—二氯乙苯硝酸盐的合成与结构表征

先以间二氯苯,氯乙酰氯和咪唑为原料合成β－（1－咪唑基）－2,4－二氯－α－苯乙醇（I）,再以二卤苯为原料合成α－氯－卤代乙苯（Ⅱa-Ⅱd),然后, Ⅰ分别与Ⅱa-Ⅱd反应,生成α－α′－甲基－卤代苄氧基）β－（1－咪唑基）－2,4－二氯乙苯硝酸盐4个新化事物,产率分别为66．8％,78．5％,76．8％和81．2％,新化合物的结构经元素分析,IR和1H NMR表征。     

头孢地尼的合成

头孢地尼的合成是用2－（2－氨基噻－4－基）－2－（Z）－（乙酰氧亚氨基）乙酰氯与7－氨基－3－乙烯基－3－头孢烯－4－羧酸二苯甲酯盐酸盐进行缩合,优化反应条件后,总收率为60％。     

Stabilization Studies on Divalent Five‐Membered Rings C4H4C,C4H4Si,C4H4Ge,C4H4Sn,and C4H4Pb

Energy differences, ΔX_S‐t (X = E, H and G) (ΔX_S‐t = X_(singlet)‐X_(triplet)) between singlet (s) and triplet (t) states are calculated at B3LYP/6‐311++G (3df,2p). The DFT calculations show that the triplet state of C₄H₄C is a ground state with planar conformer respect to its corresponding nonplanar singlet state. Both singlet and triplet states of C₄H₄M (M = Si, Ge, Sn and Pb) have a planar conformer with the singlet ground state. Four isodesmic reactions are presented for determining the stability energies, SE. NICS calculations are carried out for C₄H₄M to determine the aromatic character.     

On synthesis, structure, and thermal stability of mercury and lead sulfates and oxide sulfates

Reactions between HgO, PbO, or PbO₂ and 2.5–95 wt.% H₂SO₄ are studied at temperatures up to the boiling point of the acid. Depending on the oxide reactant, the H₂SO₄ concentration, and synthesis temperature, HgSO₄, Hg₃O₂(SO₄), PbSO₄ and Pb₂O(SO₄) are obtained as identified reaction products. The thermal stability of HgSO₄, Hg₃O₂(SO₄), PbSO₄, Pb₂O(SO₄), and PbO₂ is examined and the results supplement and modify earlier findings. The redetermined crystal structure of Hg₃O₂(SO₄) on the basis of powder neutron diffraction data shows that its space group (P3₁) is of lower symmetry than earlier reported (P3₁2₁).     

A Novel Fused Phosphorus Heterocycle: 4-(1'''',2'''',3'''',4-Tetrahydro-1, 3, 2-benzodiazaphosphorin-2''''-sulfide)-3, 4b, 4a-thiazphosphaphenanthridine Derivative

Organophosphorus compounds are ubiquitous in nature and they have broad applications in the fields of agriculture and medicine1-4. There has been a considerably growing interest in heterocyclic compounds due to their pharmaceutical importance and extensive application in organic synthesis, and the application of heterocycles is suggested to enhance the biological activity and/or offer other diverse properties5-7. In the previous work8, we have reported that 11-ethoxycarbonylmethyl-6-oxo-3, 4…     

A Review of HER4 (ErbB4) Kinase,Its Impact on Cancer,and Its Inhibitors

HER4 is a receptor tyrosine kinase that is required for the evolution of normal body systems such as cardiovascular, nervous, and endocrine systems, especially the mammary glands. It is activated through ligand binding and activates MAPKs and PI3K/AKT pathways. HER4 is commonly expressed in many human tissues, both adult and fetal. It is important to understand the role of HER4 in the treatment of many disorders. Many studies were also conducted on the role of HER4 in tumors and its tumor suppressor function. Mostly, overexpression of HER4 kinase results in cancer development. In the present article, we reviewed the structure, location, ligands, physiological functions of HER4, and its relationship to different cancer types. HER4 inhibitors reported mainly from 2016 to the present were reviewed as well.     

3-烷基/芳基-6-(2', 4'-二氯苯基)-7H-1, 2, 4-三唑[3, 4-b]- 1, 3, 4-噻二 嗪的合成及波谱性质

以间二氯苯与氯乙酰氯反应,生成ω-氯代-2,4-二氯苯乙酮(1),再使之分别与3-烷基/芳基-4-氨基-5-巯基-1,2,4-三唑(2a～2l)反应,合成了12种新的3-烷基/芳基-6-(2',4'-二氯苯基)-7H-1,2,4-三唑并[3,4-b]1,3,4-噻二嗪(4a～4l)。利用EA,IR,^1HNMR确定了其结构,并提出该反应的可能机制。     

Synthesis and Bioactivity of Novel Aminomethyl-2-（1, 2,4-triazol）-4, 4-dimethyl-3-pentanone （ol）

3, 3-Dimethyl-1-(1,2,4-triazol)-2-butanone was treated with aqueous formaldehyde to give an additional product, and subsequent elimination by acetic anhydride yielded 4,4-dimethyl-2-(1,2,4-triazol)-1-penten-3-one. Further addition with substituted amines provideda series of (1,2,4-triazol)-4,4-dimethyl-3-pentanone, which were then reduced by KBH4 to obtaina series of (1,2,4-triazol)-4,4-dimethyl-3-pentanol. Their structures were confirmed by ^1HNMR and elemental analysis. The results of bioassay showed that the title products possess good fungicidal activities.     

二苯胺-4-偶氮磺酸盐及其树脂的制备和光、热分解性质

从二苯胺 4 重氮盐(DS)和3 甲氧基二苯胺 4 重氮盐(MDS)以及重氮树脂(DR)和硝基重氮树脂(NDR)与亚硫酸钠反应,在水溶液中制备了相应的二苯胺 4 偶氮磺酸盐DSS和MDSS(简称偶氮磺酸盐)及相应的重氮树脂的偶氮磺酸盐DRS和NDRS(简称偶氮磺酸盐树脂).对它们在水溶液和固相膜中的光、热反应进行了研究.结果表明偶氮磺酸盐与偶氮磺酸盐树脂有很好的感光性能,而热稳定性比相应的重氮盐和重氮树脂好很多,其中二苯胺上有硝基取代的偶氮磺酸盐树脂具有突出的热稳定性,其水溶液在70℃加热6h,其固相膜在100℃加热11天几乎观察不到分解.对偶氮磺酸盐及偶氮磺酸盐树脂的光、热分解机理作了初步分析.     

Alkaline Earth Transition Metal Antimonides AT4Sb12 (A = Ca,Sr, Ba; T = Fe,Ru, Os) with LaFe4P12-Structure

The title compounds were prepared by reaction of CaSb₂, SrSb₂, or BaSb₃ with the transition metals and antimony in sealed silica tubes. They crystallize with the cubic LaFe₄P₁₂-structure, which was refined from single-crystal X-ray data of CaFe₄Sb₁₂, SrRu₄Sb₁₂, and BaRu₄Sb₁₂ to residuals of R = 0.014, 0.016, and 0.014, respectively. The thermal parameters of the alkaline earth ions increase with decreasing ionic size. The Sb? Sb distances are greater in the iron compound than they are in the two ruthenium compounds. This is rationalized to be due to a larger portion of electrons in antibonding Sb? Sb states in the iron compound.     

Exploratory syntheses,structures, and photoluminescent properties of three lead multi-dimensional frameworks

Three structurally diverse Pb^II coordination complexes, [Pb₃O(OH)(4-sphth)]₂(H₂O) (1), [Pb(3,5-Hdhb)]H₂O (2), and [Pb₃(4-nphth)₂(OH)₂] (3) (4-H₃sphth, 4-sulfophthalic acid; 3,5-H₂dhb, 3,5-dihydroxybenzoic acid; 4-H₂nphth, 4-nitrophthalic acid), were synthesized under hydrothermal conditions. X-ray diffraction analyses reveal that 1 is constructed from [Pb₄O₄] cubanes, based on which ladder-shaped structure is built via 4-H₃sphth bridge. This is the first Pb₄O₄-containing polymer. The Pb₂O₂ units in 2 are bridged by two parallel 3,5-HDHB ligands along the a-axis and two other parallel 3,5-HDHB ligands along the b-axis, forming a 3-D framework. For 3, the crystal structure is built up of a layer motif consisting of corner-sharing pyramidal Pb₃O units, which are linked through Pb corners to form a hexagonal unit. Each PbO₆ polyhedron is connected to three polyhedra (Pb₃O) via sharing an edge (two μ ₃-oxygen atoms) and two faces (three μ ₃-oxygen atoms), thus yielding an infinite 2-D Pb–O–Pb (3,6-net) honeycomb layer. The luminescence of 1–3 demonstrates that they may be good candidates for luminescent materials.     

Preparation, characterization of Mo, Ag-loaded BiVO4 and comparison of their degradation of methylene blue

Two types of metal-loaded visible-light-driven photocatalysts,Mo-BiVO4and Ag-BiVO4,were synthesized by wet impregnation method.Material poperties were characterized by UV-vis diffuse reflectance spectroscopy,X-ray diffraction,field emission scanning electron microscopy,X-ray photoelectron spectroscopy and low temperature nitrogen adsorption-desorption.Photocatalytic activity of the obtained materials was investigated through degrading methylene blue(MB) solution under visible-light irradiation.The results reveal that both metal loaded-BiVO4catalysts have monoclinic scheelite structure.Mo and Ag exist as oxides on the surface of the particles.The changes of absorption in visible-light region,band gap(E g) and specific surface area(A BET) caused by loading Ag are more obvious than those caused by loading Mo.But the isoelectric point of Ag-BiVO4decreases less than that of Mo-BiVO4does.Both catalysts show higher photocatalytic activity than pure BiVO4,resulting in the significantly improved efficiency of degradation of MB.And the degradation efficiency of these two metal-loaded BiVO4photocatalysts is similar to each other.However,mechanisms of such enhancement are different.The decrease of isoelectric point helps Mo-BiVO4improve the degradation efficiency.As for Ag-BiVO4,the augmentation of absorption in visible-light region as well as the abatement of E g plays more important roles.