Derivatives for Evaluation as Antineoplastic and Radioprotective Agents

Abstract

The thesis involves a review covering synthesis, chemical reactions and biological activities of thieno[2,3-d]pyrimidines. The review covers the main general methods used for preparation of thieno[2,3-d] pyrimid­ ine derivatives. In this study 5-amino-3-methyl-thiophene-2,4-dicarboxylic acid diethyl ester (I) and 5-isothiocyanato-3-methyl-thiophene-2,4-dicarbox­ ylic acid diethyl ester (II) were prepared according to reported methods and the following new compounds were prepared through the following four schemes :

Scheme (1):

I) 5-Methoxythiocarbonylamino-3-methyl thiophene-2,4-dicarboxylic acid diethyl ester (III). 2) 5-Ethoxythiocarbonylamino-3-methylthiophene-2,4-dicarboxylic acid diethyl ester (IV). 3) 5-(2-Hydroxyethoxythiocarbonylamino)-3-methyl-thiophene -2,4- dicarboxylic acid diethyl ester (V). 4) 3-Methyl-5-(3-methylthioureido) thiophene-2,4-dicarboxylic acid diethyl ester (VI). 5) 3,5-Dimethyl-4-oxo-2-thioxo-1 ,2,3,4- tetrahydrothieno [2,3-d]­

pyrimidine-6-carboxylic acid ethyl ester (VII).

6) 7-Methyl-8-oxo-2-thioxo-1 ,2,3,8-tetrahydro [I ,2,4] triazo1o[l ,5,a]­

thieno[2,3-d]- pyrimidine-6-carboxylic acid ethyl ester (IX).

7) 5-[3-(4Methylphenyl)thioureido]-3-methylthiophene-2,4- dicarboxylic acid diethyl ester (X).