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• W2331771381 abstract "One pot three component cyclocondensation of 2-amino-4-phenyl thiazole, ethyl benzoyl acetate and aromatic aldehydes produces Thiazolo Pyrimidine in moderate to good yields. Some of the compounds were screened for anti-bacterial (Staphylococcus aureus, Staphylococcus aureus (MRSA), Streptococcus pyogenes) and antifungal (Aspergillus niger) studies by Agar Diffusion method. Compounds show moderate to good antifungal activity but low antibacterial activity. INTRODUCTION Various 2-amino thiazole derivatives are of great importance to chemists as well as biologists as they exhibit a variety of biological activities like antibacterial1, antiviral2, anti-inflammatory3, antiallergies4 and antihypertensive5. The high scientific interest attracted by 3,4-dihydropyrimidines is due to broad spectrum of biological activities exhibited by these compounds like antihypertensive6, antioxidant agents7, antitumor activity8 and calcium channel modulation9. In 1893, Italian Chemist Pietro Bignelli10 synthesized 3,4-dihydropyrimidin-2(1H)-ones by heating a mixture of aldehyde, β-ketoester and urea in ethanol containing a catalytic amount of HCl. However, this procedure suffers from harsh reaction conditions, long reaction time and frequently low yield. Later on subsequent multistep synthesis furnished some what higher yield but these do not have the simplicity of original one pot protocol11. This paper reports a novel approach to the synthesis of thiazolo-pyrimidines. As thiazolo pyrimidines are classes of fused heterocycles that are of considerable interest because of their wide range of biological activities like anti cancer12, phosphate inhibitors13, antimicrobial14 and acetylcholinesterase inhibitors15. Various methods have been reported for the synthesis of thiazolo pyrimidine in literature16 which are associated with many drawbacks like multistep synthetic root, longer reaction time with drastic conditions, difficult workup, unsatisfactory yields and use of expensive & hazardous chemicals. Hence, here we report herein a general, single step and efficient approach towards the synthesis of thiazolo pyrimidines. Prompted by the observed biological activities of the above mentioned derivatives and in continuation of our research for thiazolo pyrimidines17, a rapid and efficient synthesis of a series of novel thiazolo pyrimidines and evaluation of their antimicrobial potency is being reported. RESULTS AND DISCUSSION Synthesis and characterization In view of the recent emphasis aimed at developing simple, highly efficient and one pot methodologies for the preparation of organic compounds, herein we report convergent one pot cyclocondensation of ethyl benzoyl acetate 1 ( 0.01 mole), thiazole 2 (0.01 mole), various substituted aromatic aldehydes 3 (0.01 mole) which give thiazolo pyrimidines 4 (Scheme 1). A variety of aromatic aldehydes carrying either electron donating or electron withdrawing substituents reacted very well, giving products in high purity. Scheme 1: synthesis of thiazolo pyrimidine" @default.
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• W2331771381 date "2011-10-01" @default.
• W2331771381 modified "2023-09-24" @default.
• W2331771381 title "Convergent One Pot Synthesis of Novel Thiazolo Pyrimidine and Their Antimicrobial Activities" @default.
• W2331771381 doi "https://doi.org/10.15373/2249555x/jan2014/30" @default.
• W2331771381 hasPublicationYear "2011" @default.
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