.beta.-Adrenergic blocking agents: substituted phenylalkanolamines. Effect of side-chain length on .beta.-blocking potency in vitro
摘要:
The synthesis of a group of potential beta-blockers bearing a new 5-ethoxysalicylamide substituent on nitrogen is described. These compounds were tested for beta-adrenergic blocking potency in vitro and compared with analogous compounds bearing a tert-butyl group on nitrogen. The new N-substituent increased the beta-blocking potency substantially. In a series of five homologous compounds of the type Ar(CH2)nCHOHCH2NHR (R = 5-ethoxysalicylamide; n = 0-4), two maxima of beta-blocking potency were found for n = 0 and 2. Moreover, the carbon isostere of the corresponding (aryloxy)propanolamine still proved to be a very potent beta-blocker. The ether oxygen in the side chain is therefore not an absolute requirement for activity. Structure-activity relationships are discussed.
[EN] IRON BISPHENOLATE COMPLEXES AND METHODS OF USE AND SYNTHESIS THEREOF<br/>[FR] COMPLEXES BISPHÉNOLATES DE FER ET LEURS PROCÉDÉS D'UTILISATION ET DE SYNTHÈSE
申请人:UNIV PRINCE EDWARD ISLAND
公开号:WO2013053046A1
公开(公告)日:2013-04-18
The present application, relates to iron bisphenolate complexes and methods of use and synthesis thereof. The iron complexes are prepared from tridentate or tetradentate ligands of Formula I: wherein R1 and R2 are as defined herein. Also provided are methods and processes of using the iron bisphenolate complexes as catalysts in cross-coupling reactions and in controlled radical polymerizations.
A Facile Synthesis of 4-Benzylpyridines by Regiospecific Addition of Substituted Benzylic Griganard Reagents to Pyridinium Salts
作者:Min-Jen Shiao、Win-Long Chia
DOI:10.1080/00397919108016762
日期:1991.2
Abstract Substituted 4-benzylpyridines are prepared by regiospecific γ-addition of substituted benzylic Grinard reagents to pyridinium salts in fairly good yeilds.
Development of the Vinylogous Pictet–Spengler Cyclization and Total Synthesis of (±)‐Lundurine A
作者:Aaron Nash、Xiangbing Qi、Pradip Maity、Kyle Owens、Uttam K. Tambar
DOI:10.1002/anie.201803702
日期:2018.6.4
A novel vinylogous Pictet–Spengler cyclization has been developed for the generation of indole‐annulated medium‐sized rings. The method enables the synthesis of tetrahydroazocinoindoles with a fully substituted carbon center, a prevalent structural motif in many biologically active alkaloids. The strategy has been applied to the total synthesis of (±)‐lundurine A.
The invention encompasses compounds of Formula I, including pharmaceutically acceptable salts and solvates, their pharmaceutical compositions, and their use in treating disorders associated with an excess or imbalance of tachykinins or serotonin or both.
Total Syntheses of the 3<i>H</i>-Pyrrolo[2,3-<i>c</i>]quinolone-Containing Alkaloids Marinoquinolines A–F, K, and Aplidiopsamine A Using a Palladium-Catalyzed Ullmann Cross-Coupling/Reductive Cyclization Pathway
作者:Benoit Bolte、Christopher S. Bryan、Phillip P. Sharp、Soheil Sayyahi、Charly Rihouey、Amy Kendrick、Ping Lan、Martin G. Banwell、Colin J. Jackson、Nicholas J. Fraser、Anthony C. Willis、Jas S. Ward
DOI:10.1021/acs.joc.9b02725
日期:2020.1.17
of the marinoquinoline family of natural products, together with the related marine alkaloid aplidiopsamine A (12), have been synthesized using various combinations of palladium-catalyzed Ullmann cross-coupling and reductivecyclization processes involving a C3-arylated pyrrole as the common intermediate. These natural products have been characterized by single-crystal X-ray analyses and evaluated as