Benzothiopyranoindazoles, a new class of chromophore modified anthracenedione anticancer agents. Synthesis and activity against murine leukemias
作者:H. D. Hollis Showalter、Mario M. Angelo、Ellen M. Berman、Gerald D. Kanter、Daniel F. Ortwine、Suzanne G. Ross-Kesten、Anthony D. Sercel、William R. Turner、Leslie M. Werbel
DOI:10.1021/jm00403a009
日期:1988.8
with 8-OH and 9-OH most favorable, and (c) sulfide oxidation state at S-6. Besides having curative activity against the P388 line, the more active compounds were curative against murine B-16 melanoma in vivo. On the basis of their exceptional broad-spectrum in vivo anticancer activity, selected compounds in this series have been chosen for development toward clinical trials.
描述了苯并硫代吡喃并吲哚类化合物的合成,苯并硫代吡喃并吲哚类是与米托蒽醌有关的新型生色团修饰的蒽二酮。在该结构类别中,已设计出认为是蒽环类药物的心脏毒性负责的醌部分。苯并硫代吡喃并吲哚的合成是从所需的1-氯-4-硝基-9H-噻吨黄酮-9-前体通过多步序列进行的。与单烷基肼反应得到5-硝基苯并硫代吡喃并吲哚加合物,将其催化还原成相应的C-5苯胺中间体。用必需的X(CH2)nNR1R2(X = Cl,Br; R1,R2 = H,烷基,酰基; n = 2,3)进行7烷基化可提供目标“两臂”苯并硫代吡喃并吲哚或A环甲氧基和/或侧链酰基中间体 可以通过适当的脱保护方法将其转换为3。另外,某些目标化合物3是通过将7与适当官能化的甘氨酸前体在Schotten-Bauman或BOP氯化物缩合条件下反应合成的,以提供C-5酰氨基中间体,然后进行Red-Al还原和脱保护步骤。还描述了在C-5具有近端酰基氨基侧
1,3,6,7,9,11,14,15,17,19,22,23,25,27,30,34-Hexadecaazanonacyclo-[25.5.3.2<sup>6,9</sup>.2<sup>14,17</sup>.2<sup>22,25</sup>.1<sup>3,7</sup>.1<sup>11,15</sup>.1<sup>19,23</sup>.0<sup>30,34</sup>]-tetratetracontane
作者:Johannes Dale、Christian Rømming、M. Rachel Suissa
DOI:10.1039/c39950001633
日期:——
1,1-Bis-(2-aminoethyl)hydrazine condenses with formaldehyde to a polymer that is isomerized to the nonacyclic title compound, showing increased conformational mobility and crystallizing as a tetrahydrate for which the X-ray analysis reveals channels formed by stacked rings and filled by chains of water molecules.
1,1-双(2-氨基乙基)肼与甲醛缩合成聚合物,聚合物异构化为非环状的标题化合物,显示出更高的构象流动性,并结晶为四水合物,其 X 射线分析显示出由堆叠环形成的通道,并由水分子链填充。
Substituted 1,2,4-triazine-3-methanamines
申请人:The Dow Chemical Company
公开号:US04002625A1
公开(公告)日:1977-01-11
Novel N-(phenyl)-1,4,5,6-tetrahydro-1,2,4-triazine-3-methanamines are disclosed which are useful as herbicides, insecticides, and antimicrobial agents. Various member compounds are also pharmacologically active.
本发明揭示了一种新型N-(苯基)-1,4,5,6-四氢-1,2,4-三嗪-3-甲胺类化合物,可用作除草剂、杀虫剂和抗微生物剂。此外,各种成员化合物也具有药理活性。
A comparative synthesis of 6-benzyl-2,3-dihydroimidazo[2,1-a]phthalazine and 2H-7-benzyl-3,4-dihydropyrimido[2,1-a]phthalazine
作者:Javier Munín、Lourdes Santana、Eugenio Uriarte、Fernanda Borges、Elías Quezada
DOI:10.1016/j.tetlet.2014.12.121
日期:2015.2
Two new synthetic strategies have been developed for the synthesis of a new class of cyclophthalazine derivatives. 6-Benzyl-2,3-dihydroimidazo[2,1-a]phthalazine and 2H-7-benzyl-3,4-dihydropyrimido[2,1-a]phthalazine were obtained (i) by intramolecular cyclization of the 2-(aminoalkyl)-4-benzyl-2H-phthalazin-1-one or (ii) by intramolecular cyclization of the corresponding 2-(4-benzylphthalazin-1(2H)-y
已经开发出两种新的合成策略来合成新型的环酞嗪衍生物。(i)通过2-的分子内环化获得6-苄基-2,3-二氢咪唑并[ 2,1 - a ]酞嗪和2 H -7-苄基-3,4-二氢嘧啶基[ 2,1 - a ]酞嗪。 (氨基烷基)-4-苄基-2 H-酞嗪-1-酮或(ii)通过分子内环化先前制备的相应的2-(4-苄基酞嗪-1(2 H)-亚烷基氨基)醇。所描述的第二种路线以高收率提供了所需的衍生物。