Novel synthesis of a conformationally-constrained analog of DDATHF
摘要:
A conformationally-constrained analog of DDATHF, in which the glutamate moiety is tied back to the benzoyl ring through an isoindolinone ring has been synthesized through a series of steps which commence with a Diels-Alder reaction of the Danishefsky diene with 4,4-diethoxybut-2-ynal. (C) 1997, Elsevier Science Ltd. All rights reserved.
[EN] HYDANTOIN DERIVATIVES FOR THE TREATMENT OF INFLAMMATORY DISORDERS<br/>[FR] DÉRIVÉS D' HYDANTOINE POUR LE TRAITEMENT DE TROUBLES INFLAMMATOIRES
申请人:SCHERING CORP
公开号:WO2006019768A1
公开(公告)日:2006-02-23
This invention relates to compounds of Formula (1) or a pharmaceutically acceptable salt, solvate or isomer thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, TNF- or combinations thereof.
variety of amines and for the elaboration of complex molecular architectures. Nevertheless, literature generally describes their synthesis in very low yield (below 5%), mainly due to the inefficiency of the last oxidation step. In this paper, we report a reliable synthesis of 4-substituted-ortho-phthalaldehyde analogues in 51% overall yield owing to the addition of a protecting step of the unstable
COMPOUNDS, COMPOSITIONS AND METHODS FOR THE PREPARATION OF PEPTIDE/PROTEIN CONJUGATES
申请人:The University of Hong Kong Shenzhen Institute of Research and Innovation
公开号:US20160333115A1
公开(公告)日:2016-11-17
Compounds, compositions and methods for the preparation of peptide/protein conjugates, said method comprising a step of reacting a compound (2) represented by the formula (2) with a compound (3) represented by the formula (3) to obtain compound (1) represented by the formula (1), wherein R′ represents substituent, and R represents H or at least one substituents. Also disclosed is a kit comprising the compound.
Synthesis of novel coumarin and benzocoumarin derivatives and their biological and photophysical studies
作者:Alaa S. Abd-El-Aziz、Hany M. Mohamed、Shawkat Mohammed、Shamsulhaq Zahid、Athar Ata、Ahmed H. Bedair、Ahmed M. El-Agrody、Pierre D. Harvey
DOI:10.1002/jhet.5570440610
日期:2007.11
The reaction of 1-chloromethylbenzo[f]coumarins (36) with cyanide anion under different reaction conditions was also investigated in order to assess its suitability for nucleophilic substitution reactions as well as ring transformation products (43-49). Synthesis of 1-((benzo[d]thiazol-2-yl)methyl)-9-hydroxybenzo[f]coumarin (50) represented the first example of methylene bridge-head heterocyclecontaining
通过香豆素-3-羰基氯(1)与许多亲核试剂的反应已经制备了香豆素-3 N-羧酰胺的几种衍生物(3-21)。还使用相同的方法制备了新型双头香豆素-3 N-羧酰胺(26-33)。应用Pechmann-Duisberg反应制备新的苯并[ f ]-苯并[ h ]香豆素和4-(氯甲基)-吡喃并[3,2 - c ]香豆素-2-酮(36-42)。1-氯甲基苯并[ f ]香豆素的反应(36)还研究了在不同反应条件下与氰化物阴离子形成的阴离子,以评估其对亲核取代反应以及环转化产物的适用性(43-49)。1-((苯并[ d ]噻唑-2-基)甲基)-9-羟基苯并[ f ]香豆素(50)的合成代表了含亚甲基桥头杂环的苯并[ f ]香豆素的第一个实例。一些新制备的香豆素对革兰氏阳性和革兰氏阴性细菌表现出抗菌活性。发现化合物36d对所有经筛选的细菌具有活性。对选定的荧光苯并[ f ]-和苯并[ h ]进行了光物理研究
An Unusual Synthesis of Phthalaldehyde
作者:Ernest Wenkert、Haripada Khatuya
DOI:10.1080/00397919908086247
日期:1999.7
Abstract A variety of oxidizing agents convert 5-hydroxy-4,5-dihydroisobenzo-furan into phthalaldehyde. Other oxidizing agents produce both phthalaldehyde and its 4-hydroxy derivative.