二胺与二酮环聚合反应的不同途径与产物

在质子性溶剂中,3,5-二叔丁基-1,2-苯醌分别与双[(三异丙基硅烷基)乙炔基]萘-2,3-二胺和双[(三异丙基硅烷基)乙炔基]蒽-2,3-二胺反应,在不同条件下得到含有吡嗪环的缩合产物1和含有咪唑环的缩合产物2.通过核磁共振波谱、紫外-可见光谱、高分辨质谱及单晶X射线衍射表征确定了产物的结构,并提出了可能的反应机理.

The Triazole and Thiophene Containing New Heterocyclic Systems

The aim of the current work is to create new heterocyclic tetracyclic condensed systems which combine benzothiofen and benzimidazoleinto one molecule. The haisic products are 1,2-, 2,3- and 3,4- diamines of dibenzothiophenes. Orto-diamines react with hydrochloric acid and sodium nitrite and obtain three new isomeric heterocyclic systems： 3H-benzothieno[3,2-e]benzotriazole, 3H-benzothieno[2,3-f]benzotriazole and 1H-benzothieno[3,2-g]benzotriazole with the anticipated biological activity. Their spectral characteristics are studied.

Crystal and Molecular Structure of Methylene-bis[benzobicyclo(diaza-diphenyl) stannoxide],[o-O■n(C_6H_5)_2]_2CH_2·1/2C_6H_6

Methylene-bis[benzobicyclo(diaza-diphenyl) stannoxide,C_(41)H_(34)N_4O_4Sn_2·1/2C_6H_6],Mr=923.19,m.p.126-127℃,triclinic,P1,a=9.780(4),b=14.485(2),c=15.122(6),α=74. 95(3),β=72.21(3),γ=82.68(2)°,V=1967(1) Z=2,Dx=1.56 g/cm￣3, MoKα(λ=0.71073),μ=13.20 cm-1,F(000)=922;final R=0.045, Rw=0.046 for 3637 observed reflections(I≥3σ(I)).The title compound is a bimetallo-heterocyclic complex prepared by condensation.Each tin atom has a trigonal bipyramidal coordination with two oxygen atoms occupying the axial positions.

Synthesis and Structure of a Novel Macrocyclic Ligand( C_(22) H_(29) N_3 O_3 Br_2)

The title compound, 1,12,15 triaza 3,4:9,10 dibenzo 5,8 dioxacyclopentadecane N acetic lactam (C 22 H 29 N 3O 3Br 2, M r =543.29) has been synthesized and characterized by analytical data, IR and 1HNMR spectra. The compound crystallizes in the trigonal system, space group R 3 with a = 35.194(1), c = 10.397(1) , γ=120°, V=11152.6(1) 3, Z=18, D c =1.456 gcm -3 , F(000)=4968, μ =3.3 mm -1 . Mo Kα radiation ( λ = 0.71073), R = 0.0145 for 3094 observed reflections 〔 I>2σ(I )〕 of 3392 independent reflections. The result shows that monofunction reaction for polyaza macrocycle were protonized. 1H NMR spectra of the ligand showed two sets of multiplets due to the two phenyl rings of the ligand in different environments.

Spirogen公司与Genentech公司联合开发抗体-药物结合物类抗癌药

专门研发DNA序列靶向抗癌药的英国Spirogen公司目前已与Genenteeh公司达成合作协议，使用Spirogen公司研制的吡咯并苯并二氮杂革类（PBDs）药物及相关键合技术，共同开发抗体一药物结合物（ADCs）类抗癌药。ADCs是由一种特异性单克隆抗体与一种化疗药物键合而成，其将抗体的靶向性和细胞毒药物的抗癌活性融于一身，更具肿瘤的靶向治疗活性，降低了传统化疗药物的毒副作用。