Synthesis of substituted arylguanidines as potential drugs VI.

S Y N T H E S I S O F S U B S T I T U E D A R Y L G U A N I D I N E S A S P O T E N T I A L D R U G S V I . Author: Korábečný J. Tutor: Palát K. Dept. of Inorganic and Organic Chemistry Faculty of Pharmacy in Hradec Kralové Charles University in Prague, Czech Republic Background: High number of life imperilling mycotic infection carries with itself increased need of antifungal drugs and need of new substances. In usage of antimycobacterial drugs it is also the same. Increasing resistance of pathogenic organisms urges human population to search for new, effective drugs. Aim of study: The aim of my diploma work was to prepare series of substitued arylguanidines, mainly 1-[3-chlor-4- (alkylsulfanyl)phenyl]guanidines, which are tested on antifungal and antimycobacterial activity. Methods: 2-Chloro-1-(alkylsulfanyl)-4-nitrobenzenes were synthesized from 3,4-dichloronitrobenzene by custom methods; either by using of active copper or by using Pd2(dba)3 and Xantphos as catalyzers. The following reduction of nitrogroup to aminogroup was made by stannous chloride under nitrogen atmosphere. Rise of appropriate amonnium salts proceeded in reaction with gaseous dry hydrogen chloride, almost quantitatively. Reaction leading to rise of guanidines proceeded with cyanamide in the melt or ethanolic solution in autoclave at..