呋喃环开环-吡咯环闭环:芳基(杂芳基)环化吡咯并[1,2- a ] [1,4]二氮杂pine的新合成途径†
摘要:
描述了吡咯并[1,2- a ] [1,4]苯并二氮杂s的合成方法。该方法是基于用Na 2 O 3处理的N-(糠基)蒽酰胺的再循环。盐酸/醋酸 系统,并允许两者同时形成 地西平和吡咯环一步就形成。反应通过 呋喃开环成二酮部分,随后NH 2-基团与两个羰基官能团连续相互作用。由于竞争性糠基阳离子消除,该方法在酰胺氮上存在烷基或芳基的情况下效率不高。但是吡咯并[1,2- a ] [1,4]苯并二氮杂卓的烷基化有效地产生了相应的N-烷基衍生物。在这些反应条件下,由于二氮杂ring环形成的可逆性,立体效应也阻止了环化作用。但是,相应的吡咯并[1,2- a ] [1,4]苯并二氮杂卓可通过逐步方法获得,即1)呋喃环开环为aq。盐酸/醋酸 和2)在冰河处理下,将分离的氨基二酮环化 醋酸。合成吡咯并[1,2- a ] [1,4]苯并二氮杂卓的另一种有效方法是酸催化N-(糠基)-2-硝基苯甲酰胺的呋喃环开环,然后处理所形成的吡咯并[1
Synthesis and properties of 1,2-dihydro-4(3H)-quinazolinones
作者:D. S. Khachatryan、S. K. Belus、V. A. Misyurin、M. A. Baryshnikova、A. V. Kolotaev、K. R. Matevosyan
DOI:10.1007/s11172-017-1852-2
日期:2017.6
We modified the preparative-scale method for the synthesis of 2-aryl 1,2-dihydro-4(3H)-quinazolinone derivatives obtained in high yields by the reaction of new and commercially available aromatic aldehydes with anthranilic acid amides. A series of quinazolinone derivatives possessing anticancer and antiparasitic activities, as well as capable of preventing the progress of neurodegenerative diseases
Synthesis of Isoindolo[2,1-<i>a</i>]quinazoline Derivatives in Ionic Liquid Catalyzed by Iodine
作者:Lian Lu、Ke Yang、Mei-Mei Zhang、Xiang-Shan Wang
DOI:10.1002/jhet.1696
日期:2014.5
A mild, green, and facile method for the synthesis of 6,6a‐dihydroisoindolo[2,1‐a]quinazoline‐5,11‐dione derivatives is described in high yields using ionicliquids as green media. The method involves the reaction of 2‐aminobenzamides with 2‐formylbenzoic acid catalyzed by iodine and provides a new alkaloid library with potential activity for biomedical screening.
申请人:The United States of America, as Represented by the Secretary, Dept. of Health & Human Services
公开号:US20150119426A1
公开(公告)日:2015-04-30
Disclosed are modulators of the human relaxin receptor 1, for example, of formula (I), wherein A, R
1
, and R
2
are as defined herein, that are useful in treating mammalian relaxin receptor 1 mediated facets of human health, e.g., cardiovascular disease. Also disclosed is a composition comprising a pharmaceutically suitable carrier and at least one compound of the disclosure, and a method for therapeutic intervention in a facet of mammalian health that is mediated by a human relaxin receptor 1.
transformations are based on the fact that DMF can serve as a reaction solvent and one carbon synthon for the construction of heterocyclic rings. Moreover, this protocol features base-free and Brønsted acid free environmentally benign conditions with broad synthetic scope. A good scalability is demonstrated.
An Efficient Synthesis of Pyrrolo[1,2-<i>a</i>]quinazoline Derivatives in Ionic Liquid Catalyzed by Iodine
作者:Lian Lu、Ke Yang、Mei-Mei Zhang、Xiang-Shan Wang
DOI:10.1002/jhet.1116
日期:2014.5
A mild, green, and facile method for the synthesis of 2,3,3a,4‐tetrahydropyrrolo[1,2‐a]quinazoline‐1,5‐dione derivatives is described in high yields by using ionicliquids as green media. The method involves the reaction of 2‐aminobenzamides with 4‐oxopentanoic acid or 4‐aryl‐4‐oxo‐butanoic acid catalyzed by iodine and has the advantages of mild reaction conditions, high yields, one‐pot, operational
以离子液体为绿色介质,高收率地描述了一种温和,绿色且简便的合成2,3,3 a,4-四氢吡咯并[1,2 - a ]喹唑啉-1,5-二酮衍生物的方法。该方法涉及2-氨基苯甲酰胺与碘催化的4-氧代戊酸或4-芳基-4-氧代丁酸的反应,具有反应条件温和,收率高,单反应釜,操作简便和对环境无害的优点。 。