5411-61-0Relevant academic research and scientific papers
Grob-Type Fragmentation Releases Paracyclophane Ring Strain in a Late-Stage Precursor of Haouamine A
Cao, Liming,Wang, Chenbo,Wipf, Peter
supporting information, p. 1538 - 1541 (2019/03/08)
A ketene [2 + 2]-addition, an intramolecular aldol reaction, a Suzuki-Miyaura coupling, and a chemoselective lactam reduction were used to prepare a late-stage precursor of haouamine A. Exposure to acid led to a Grob-type fragmentation of the strained 3-aza[7]paracyclophane ring, followed by a tandem Pictet-Spengler reaction of the intermediate iminium ion and conversion to a novel 1,4a-propanocyclopenta[b]pyridine. This cascade reaction might also be relevant for the mechanism of action of the natural product.
Development of 3,4-dihydroisoquinolin-1(2H)-one derivatives for the Positron Emission Tomography (PET) imaging of σ2 receptors
Abate, Carmen,Selivanova, Svetlana V.,Müller, Adrienne,Kr?mer, Stefanie D.,Schibli, Roger,Marottoli, Roberta,Perrone, Roberto,Berardi, Francesco,Niso, Mauro,Ametamey, Simon M.
supporting information, p. 920 - 930 (2013/11/19)
σ2 Receptors are promising biomarkers for cancer diagnosis given the relationship between the proliferative status of tumors and their density. With the aim of contributing to the research of σ2 receptor Positron Emission Tomography (PET) probes, we developed 2-[3-[6,7-dimethoxy-3,4-dihydroisoquinolin-2(1H)-yl]propyl]-3, 4-dihydroisoquinolin-1(2H)-one (3), with optimal σ2 pharmacological properties and appropriate lipophilicity. Hence, 3 served as the lead compound for the development of a series of dihydroisoquinolinones amenable to radiolabeling. Radiosynthesis for compound 26, which displayed the most appropriate σ2 profile, was developed and σ2 specific binding for the corresponding [18F]-26 was confirmed by in vitro autoradiography on rat brain slices. Despite the excellent in vitro properties, [18F]-26 could not successfully image σ2 receptors in the rat brain in vivo, maybe because of its interaction with P-gp. Nevertheless, [18F]-26 may still be worthy of further investigation for the imaging of σ2 receptors in peripheral tumors devoid of P-gp overexpression.
CYCLIC AMINE DERIVATIVE OR SALT THEREOF
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Page/Page column 24-25; 48, (2010/11/27)
Provided are compounds which are an NMDA antagonist having a broad safety margin and are useful as a treating agent or a preventing agent for Alzheimer's disease, cerebrovascular dementia, Parkinson's disease, ischemic apoplexy, pain, etc. Concretely prov
5-HT SELECTIVE AGENTS
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, (2008/06/13)
Substituted 8-alkoxy-1,2,3,3a,8,8a-hexahydroindeno[1,2-c] pyrroles; 5-alkoxy-2,3,4,4a,9,9a-hexahydro-1H-indeno[2,1-c]pyridines; and 9-alkoxy-2,3, 3a,4,5,9a-hexahydro-1H-benz[e]isoindoles are selective 5-HT receptor agents and are thus useful in the treatm
Synthesis and structure activity relationships of cis- and trans- 2,3,4,4a,9,9a-hexahydro-1H-indeno[2,1-c]pyridines for 5-HT receptor subtypes
Meyer,DeBernardis,Hancock
, p. 105 - 112 (2007/10/02)
A series of cis- and trans-fused hexahydroindeno[2,1-c]pyridines have been prepared and evaluated for affinity and selectivity at the 5-HT(1A) subtype of the serotonin receptor. Using molecular modeling studies we predicted that the 5-methoxy-trans-fused
5-HT selective agents
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, (2008/06/13)
Substituted 8-alkoxy-1,2,3,3a,8,8a-hexahydroindeno-[1,2-c]pyrroles; 5-alkoxy-2,3,4,4a,9,9a-hexahydro-1H-indeno[2,1-c]pyridines; and 9-alkoxy-2,3,3a,4,5,9a-hexahydro-1H-benz[e]isoindoles are selective 5-HT receptor agents and are thus useful in the treatment of anxiety, depression, and hypertension.
Marine Bacteria, II. - Synthesis of Cyclic and Steric Hindered Pseudilines
Pudleiner, Heinz,Laatsch, Hartmut
, p. 423 - 432 (2007/10/02)
For structure-activity studies, various derivatives of pentabromopseudiline (1) were synthesized with distorted (3a) or hetero-cis-arranged rings (30c).The pyrrole 30c was accessible by Paal-Knorr cyclization of the 4-keto aldehyde 25d, which was obtained
