Abstract:
The synthesis ofthe fused pyrimidine is divided into two headings: such as; annelated
substrate and annelating reagent. The annelating substrate artha-amino ester as ethyl-
5-amino-l-methylpyrazol-4-carboxylate (2), which was prepared from
8
14).R=-@
IS). R = - Si(Cl-j)3
16). R = - Cli - OH
17). R~ - (CIi)3 - CH:J
COOEt
N~C=C-R
I
Me
4
ethyl(ethoxymethylene)cyanoacetate by usmg Gewald procedure and annelating
reagents as 2-methylthio-2-methylthiazoline (7) and 2-methylthio-imidazoline (11),
which were synthesized from ethanol amine (5) and diethylamine (9) by using Jensen
& Hofmann method. The annelating substrate (2) was used in the synthesis of 1-
methyl-4-oxo-5-(p-toluoyl)-pyrazolo[3,4-djpyrimidin (4). The annelating substrate
(2) was used to synthesize l-rriethyl-6,7-dihydropyrazolo[3,4-djthiazolo[I,2-
ajpyrimidine-4-one (8) and l-methyl-6,7-dihydropyrazolo[3,4-djimidazo(l,2-
ajpyrimidin-4(8H)-one (12) by one step reaction in dry acetic acid. The compounds
ethyl-5-iodo-l-methylpyrazol-4-carboxylate (13), ethyl-5-phenylethynyl-lmethylpyrazol-
4-carboxy late (14), ethy1-5-trimethylsilylethynyl-l-methylpyrazol-4-
carboxylate (15), ethyl-5-propynylol-l-methylpyrazol-4-carboxylate (16) and ethyl-5-
hexayne-l-methylpyrazol-4-carboxylate (17) were synthesized from annelating
substrate (2). In vitro antimicrobial activity of fused primidine and 5-alkynyl pyrazol
derivatives were evaluated. All the synthesized compounds demonstrated mild growth
inhibition against antibiotic-susceptible standard and clinically isolated strains of
gram-positive and gram-negative bacteria as well as human fungal pathogens.
