Synthesis and Biological Activity of Phencyclidine Homologues with para-Hydroxy-Group in the Aromatic Ring.

ChemInform ◽  
2005 ◽  
Vol 36 (34) ◽  
Author(s):  
V. A. Glushkov ◽  
L. V. Anikina ◽  
Yu. B. Vikharev ◽  
O. G. Stryapunina ◽  
Yu. V. Shklyaev ◽  
...  
ACS Omega ◽  
2021 ◽  
Vol 6 (5) ◽  
pp. 3717-3726
Author(s):  
Manoj Kushwaha ◽  
Arem Qayum ◽  
Shreyans K. Jain ◽  
Jasvinder Singh ◽  
Amit Kumar Srivastava ◽  
...  

Molecules ◽  
2018 ◽  
Vol 24 (1) ◽  
pp. 57 ◽  
Author(s):  
Olga Ivanova ◽  
Vladimir Andronov ◽  
Irina Levina ◽  
Alexey Chagarovskiy ◽  
Leonid Voskressensky ◽  
...  

A simple method has been developed for the synthesis of cyclopropa[c]coumarins, which belong to the donor-acceptor cyclopropane family and, therefore, are promising substrates for the preparation of chromene-based fine chemicals. The method, based on the acetic acid-induced intramolecular transesterification of 2-arylcyclopropane-1,1-dicarboxylates, was found to be efficient for substrates containing hydroxy group directly attached to the aromatic ring.


2000 ◽  
Vol 65 (1) ◽  
pp. 77-82 ◽  
Author(s):  
Suzana Jovanović-Šanta ◽  
Silvana Andrić ◽  
Radmila Kovačević ◽  
Vjera Pejanović

Starting from estrone 3-benzyloxy-17β-hydroxyestra-1,3,5(10)-trien-16-one oxime (3b) was synthesized, which underwent Beckmann fragmentation giving the 3-benzyloxy-17-oxo- 16,17-secoestra-1,3,5(10)-triene-16-nitrile (4b). Sodium borohydride reduction of this compound afforded 3-benzyloxy-17-hydroxy-16,17-secoestra-1,3,5(10)-triene-16-nitrile (5b). The deprotection of the 3-hydroxy group was achieved by action of hydrogen upon derivatives 4b and 5b in presence of Pd/C as a catalyst, yielding 3-hydroxy-17-oxo-16,17-secoestra- 1,3,5(10)-triene-16-nitrile (4a) and 3,17-dihydroxy-16,17-secoestra-1,3,5(10)-triene-16-nitrile (5a). In biological tests on experimental animals, compounds 4a, 4b, 5a and 5b showed virtually a complete loss of estrogenic activity, whereas compounds 4a, 5a and 5b exhibited moderate antiestrogenic effect.


2015 ◽  
Vol 7 (2) ◽  
pp. 73 ◽  
Author(s):  
Kevin Cannon ◽  
Deepa Gandla ◽  
Samantha Lauro ◽  
Lee Silverberg ◽  
John Tierney ◽  
...  

1,3-thiazolidin-4-ones, also known as thiazolidin-4-ones, are known to have a very wide range of biological activity. The corresponding S-oxides may show enhanced activity, and therefore viable synthetic routes to these S-oxides are required. S-oxidation of 3-cyclohexyl-2-phenyl-1,3-thiazolidin-4-ones with Oxone® was investigated. For all compounds evaluated, selective oxidation to the sulfoxide was realized using 3 equivalents of Oxone® at room temperature. Alternatively, the sulfone was prepared selectively at high temperature by increasing the equivalents of Oxone® used; the extent of this selectivity was affected by the substituent of the aromatic ring. In those cases in which the reaction produced a mixture of the sulfoxide and sulfone, the ratio of the products was quantified by 1H NMR.


2001 ◽  
Vol 7 (8) ◽  
pp. 413-424 ◽  
Author(s):  
Jiřina Slaninová ◽  
Lenka Maletínská ◽  
Jiří Vondrášek ◽  
Zdenko Procházka

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