ABSTRACT A series of novel 1,2,4-thiadiazine 1,1-dioxides were synthesized by condensation of 2-chlorobenzenesulfonamide and 4-chloropyridine-3-sulfonamide with heterocyclic methyl carbimidates obtained from heterocyclic carbonitriles and used at the time of their creation. Substituted amidines were isolated as the intermediates in the reaction with 2-chlorobenzenesulfonamide. Those intermediat...

Non-fused 3,6-dihydro-2H-1,3-thiazine-2-thiones constitute a so far rather unexplored class of compounds, with the latest report dating back more than two decades. Thiazine-2-thiones contain an endocyclic dithiocarbamate group, which is often found in pesticides, in substrates for radical chemistry and in synthetic intermediates towards thioureas and amidines. We now report the multicomponent r...

The parallel solid phase synthesis of an 18-member library of 2-substituted pyrimidines is described using a chlorogermane-functionalised resin. The success of the key Pinner-type condensations between a resin-bound enaminone and an array of amidine hydrochlorides highlights the stability of arylgermane linkers (cf. arylsilanes) towards strongly basic/nucleophilic conditions.

Titanium(IV)-mediated reactions between primary amines and secondary carboxamides exhibit different outcomes, amidine formation versus transamidation, depending on the identity of the TiIV complex used and the reaction conditions employed. The present study probes the origin of this divergent behavior. We find that stoichiometric TiIV, either Cp*TiIV complexes or Ti(NMe2)4, promotes formation o...

A library of 19 novel 4-(4-phenylpiperazine-1-yl)benzamidines has been synthesized and evaluated in vitro against Pneumocystis carinii. Among these compounds, N-ethyl- and N-hexyl-4-(4-phenylpiperazine-1-yl)benzamidines emerged as the most promising compounds, with inhibition percentages at 10.0 microg/mL of 87% and 96%, respectively. Those compounds remained active at 0.1 microg/mL.

The aryl-(Z)-N-[2-amino-1,2-dicyanovinyl]formamidine 2 cyclize in solvent-free conditions and in the presence of a base to give a 5-amino-1-aryl-4-cyanoimidazoles 3. Silica sulfuric acid as an efficient and reusable heterogeneous catalyst has been used for the preparation of amidines 2 from formimidate 1 through reaction with aromatic amines at room temperature and in good to excellent yields. ...

The aryl-(Z)-N-[2-amino-1,2-dicyanovinyl]formamidine 2 cyclize in solvent-free conditions and in the presence of a base to give a 5-amino-1-aryl-4-cyanoimidazoles 3. Silica sulfuric acid as an efficient and reusable heterogeneous catalyst has been used for the preparation of amidines 2 from formimidate 1 through reaction with aromatic amines at room temperature and in good to excellent yields. ...

Insecticides continue to be the primary means of control for ectoparasites on livestock. Intensive use of these materials has led to resistance to organochlorines, organophosphates and pyrethroids among populations of Haematobia irritans irritans, H. irritans exigua and Lucilia cuprina. Similarly, use of acaricides has led to resistance in one-host Boophilus ticks to all currently-used organoph...