邻氨基苯甲酸置于溴体系中,用 溶剂黄146 作为反应溶剂,化学反应生成 2-氨基-5-溴苯甲酸 参考文献:Quinazolinone Platinum Metal Complexes: In Silico Design,Synthesis And Evaluation Of Anticancer Activity 标题:Quinazolinone Platinum Metal Complexes: In Silico Design,Synthesis And Evaluation Of Anticancer Activity 摘要:二氢叶酸还原酶(dhfr)已被视为一种靶标,用于开发治疗各种人类疾病(包括癌症,自身免疫性疾病和传染性疾病)的药物.有几种金属复合物正被用于治疗癌症.方形平面铂(II)复合物顺式 Ptcl2(Nh3)2 在强迫丝状生长方面更为有效.顺铂是一种无机重金属复合物,其活性类似于细胞周期阶段非特异性烷化剂,如环磷酰胺和其他一些镍和铜金属复合物.它能产生链内 Dna 交联并形成 Dna 加合物,从而优先抑制 Dna,Rna 和蛋白质的合成.铂金属复合物的筛选是通过 Vlife Mds 4.3 软件进行的.筛选过程包括分子选择,Pdb 选择,Pdb 优化和分子对接.金属配合物的合成采用多组分反应法.通过 Ir,Tlc,NMR,Xrd,Fesem 和一些物理化学参数对硅学研究优先考虑的喹唑啉酮席夫碱铂金属配合物进行了表征.以阿霉素为标准,对十种细胞系进行了体外抗癌细胞系测定,进一步评估了优先分子.结果表明,坤唑啉酮席夫碱的铂金属配合物可以通过 Dhfr 抑制机制成为潜在的抗癌剂. DOI:10.14233/ajchem.2018.21330
专利号:US-5783577-A 优先权日:1995-09-15 标题 :Synthesis of quinazolinone libraries and derivatives thereof 发明人:HOUGHTEN RICHARD A; OSTRESH JOHN M 权利人:TREGA BIOSCIENCES INC 摘要:The present invention provides synthetic combinatorial libraries of organic compounds based on the quinazolinone ring.
专利号:US-9364482-B2 优先权日:2013-06-24 标 题 :Substituted benzofuran compounds and methods of use thereof for the treatment of viral diseases 发明人:DAI XING; LIU HONG; PALANI ANANDAN; HE SHUWEN; NARGUND RAVI; XIAO DONG; ZORN NICOLAS; DANG QUN; MCCOMAS CASEY C; PENG XUANJIA; LI PENG; SOLL RICHARD 权利人:MERCK SHARP & DOHME 摘要:The present invention relates to compounds of formula I that are useful as hepatitis C virus (HCV) NS5B polymerase inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5B polymerase activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system. (I)
专利号:US-11434243-B2 优先权日:2017-12-19 标 题 :Triazoloquinazolinone synthesis 发明人:JAGUSCH THOMAS; ZENHORST PETER ADRIANUS HUBERTUS; VAN DER AA PAULA ANNA ADRIANA; VERSPUI GOVERT ARIE; KAS MARTIN; SCIGELOVA MARTINA 权利人:GABATHER AB 摘要:The invention relates to an improved process for preparing triazoloquinazolinones of Formula (I),including 9-benzyl-2-(4-methylphenyl)-2,6-dihydro[1,2,4]triazolo[4,3-c]quinazoline-3,5-dione, pharmaceutical compositions comprising the compounds of Formula (I), including 9-benzyl-2-(4-methylphenyl)-2,6-dihydro[1,2,4]triazolo[4,3-c]quinazoline-3,5-dione, prepared by the improved process, and methods of treatment using the compounds of Formula (I), including 9-benzyl-2-(4-methylphenyl)-2,6-dihydro[1,2,4]triazolo[4,3-c]quinazoline-3,5-dione, prepared by the improved process.
专利号:WO-9811438-A1 优先权日:1996-09-13 标题 :Synthesis of quinazolinone libraries and derivatives thereof
专利号:US-7071145-B2 优先权日:2001-09-25 标 题:Thermosensitive recording material, and synthesis method of oligomer composition for the recording material 发明人:MORITA MITSUNOBU; HAYAKAWA KUNIO; TORII MASAFUMI; NARUSE MITSURU 权利人:RICOH KK 摘要:A thermosensitive recording material comprising a thermosensitive layer provided on a substrate, and the thermosensitive layer comprises as main ingredients a leuco dye and a developer to make colored state of said leuco dye when heated, wherein the developer is an oligomer composition obtained from the reaction of a polyvalent isocyanate compound represented by following Formula (I) with an aromatic amine represented by following Formula (II); n nwhere X represents a try- or more-valent group, a represents an integer numeral of 3 or more, b and c represent respectively integer numerals in the range of 0 to 5 and they satisfy a relation of b+c=1 to 5, Z represents hydrogen atom, alkyl group, allyl group or aryl group, and the aryl group may include condensed ling structure thereof, and d represents an integer numeral in the range of 0 to 4. This developer shows excellent reliabilities of both image and background area, and also shows an excellent color-developing characteristics (color developing sensitivity and image density).
专利号:US-2024343719-A1 优先权日:2017-03-17 标题 :Kappa opioid receptor antagonists and products and methods related thereto 发明人:ROBERTS EDWARD; GUERRERO MIGUEL A; URBANO MARIANGELA; ROSEN HUGH; JONES ROBERT M; LAXAMANA CANDACE MAE; ZHAO XIANRUI; TURTLE ERIC DOUGLAS 权利人:SCRIPPS RESEARCH INST; BLACKTHORN THERAPEUTICS INC 摘要:Compounds are provided that antagonize the kappa-opioid receptor (KOR) and products containing such compounds, as well as to methods of their use and synthesis. Such compounds have the structure of Formula (I), or a pharmaceutically acceptable isomer, racemate, hydrate, solvate, isotope or salt thereof: n n n n n n n n n n wherein X, Y, R 1 , R 2 , R 4 , R 5 R 6 , R 7 , R 8 and R 11 are as defined herein.
[参考文献]: Rafael Gozalbes, Et Al. Qsar-Based Solubility Model For Drug-Like Compounds. Bioorg Med Chem. 2010 Oct 1;18(19):7078-84.
合成参考文献
摘要:Silva, V. L. M.; Pinto, D. C. G. A.; Santos, C. M. M.; Rocha, D. H. A., Science of Synthesis Knowledge Updates, (2022) 3, 232. 摘要:Kang, F.-A.; Yang, S.-M., Science of Synthesis Knowledge Updates, (2015) 2, 190. 摘要:P. Leggate and G.E. Dunn. Can. J. Chem. 43, 1158 (1965). 摘要:P. Leggate and G. E. Dunn, Can. J. Chem. 43, 1158 (1965).