Probing phenol dimer in molecular complex: Role of nitro group and stabilizing agent

2019 ◽  
Vol 1193 ◽  
pp. 103-109 ◽  
Author(s):  
Sumit Kumar Panja ◽  
Supriy Verma ◽  
Satyen Saha
Author(s):  
Constantine D. Tsoukas ◽  
Mary Valentine ◽  
Martin Lotz ◽  
John H. Vaughan ◽  
Dennis A. Carson

Author(s):  
Douglass F. Taber

(+)-Complestatin 3 shows promising activity against HIV infectivity. Dale L. Boger of Scripps/La Jolla described (J. Am. Chem. Soc. 2010, 132, 7776) an elegant multicomponent assembly of 3, the key step of which was the atropisomer-selective intramolecular Larock cyclization of 1 to 2. The preparation of 1 began with the protected phenethylamine 5, prepared by Sharpless asymmetric aminohydroxylation of the styrene 4. Conversion of 5 to the areneboronic acid followed by coupling with 6 delivered 7. Acylation led to 8, with the stage set for nitro-assisted addition-elimination, to form the first bis-aryl ether of 3. The product was a mixture of atropisomers, subsequently symmetrized to 9 by removal of the nitro group. Acylation of 9 led to 1. The role of the silyl group on the alkyne of 1 was to direct the regioselectivity of the intramolecular Larock indole synthesis. Again, two atropisomers were possible from the cyclization. Earlier model studies had suggested some preference for one over the other. As it turned out, in this case the desired atropisomer was the only one observed. It is particularly striking that the coupling was efficient even in the presence of the readily reduced and unprotected chlorophenols. The modular nature of this route to (+)-complestatin 3 will make it possible to prepare a variety of analogues. As long as only the substituents on the periphery are changed, the atropisomer selectivity in the Larock cyclization should be maintained.


Synthesis ◽  
2020 ◽  
Author(s):  
Zbigniew Wróbel ◽  
Michał Tryniszewski ◽  
Robert Bujok ◽  
Roman Gańczarczyk

Tributyl- or triphenylphosphine promotes a one-pot, three-step method for the synthesis of differently substituted dibenzodiazepinones from N-aryl-2-nitroanilines. Pyridine analogues and the corresponding thiazepinones can also be formed using this method. The process involves deoxygenation of the nitro group, then formation of an iminophosphorane intermediate and its intramolecular condensation with a carboxyl group placed in the N-aryl group. The role of the carboxyl group in the formation of the iminophosphorane and the mode of cyclization are discussed.


2020 ◽  
Vol 992 ◽  
pp. 271-276
Author(s):  
B.M. Goltsman ◽  
L.A. Yatsenko ◽  
Elena A. Yatsenko

The prospects for the use of foam glass in construction were described. The modern compositions of foaming mixtures for foam glass synthesis were considered. Compositions for studying the influence of the foaming mixture components on the formation of foam glass porous structure were developed, their internal structure and properties were studied. The role of each component of the mixture on its foaming was revealed. Glycerol is a pore-forming agent, which decomposes and produces foaming gases. Waterglass is a stabilizing agent reducing glycerol combustion process. Recommendations on the application of the described patterns in the foam glass synthesis were given.


CNS Spectrums ◽  
2004 ◽  
Vol 9 (S1) ◽  
pp. 7-12
Author(s):  
Philip G. Janicak

Antipsychotics have been utilized in the treatment of bipolar disorder for many decades and were the mainstay of treatment before lithium was reintroduced in the late 1960s. Today, many bipolar patients who present with psychotic features are misdiagnosed and prescribed an antipsychotic for another disorder. Estimates of psychotic symptoms in bipolar disorder, particularly during a manic episode, are ≥50% by clinical assessment and even higher by individual reports. Thus, antipsychotics are frequently used: as first treatment for psychosis not recognized as bipolar disorder, and as an adjunct to a mood-stabilizing agent in bipolars with psychotic symptoms.Most recently, antipsychotics have been examined for their mood-stabilizing properties as well (Slide 9). One may conceptualize using a selective serotonin reuptake inhibitor (SSRI) antidepressant for disorders such as panic disorder or obsessive-compulsive disorder, and using an antiepileptic as a mood-stabilizing agent; however, it is more difficult to accept that an agent approved for treatment of psychosis can be a primary therapy for bipolar disorder. Data from the monotherapy trials suggest that second-generation antipsychotics (SGAs) are at least as effective as lithium and valproic acid for acute mania. There is a very large database indicating that SGAs can be utilized as monotherapy for acute mania. However, there is limited data on the role of these agents in prevention of relapse and recurrence and in their efficacy for depression in the context of bipolar disorder. More studies will be needed to clarify whether SGAs should be used as monotherapy or whether they would be best used as augmenting agents in severe and psychotically manic or depressed patients.


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