- N- vs. S-PTC alkylation of 5-carboethoxy-2-thiouracil and its reactivity towards some nucleophilic reagents
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The reactivity of 5-carboethoxy-2-thiouracil (1) toward alkylation by different organohalogen compounds under phase-transfer catalysis (PTC) conditions has been investigated to give S-monoalkylated products and/or simultaneous S- and N-dialkylated product
- Hassan,Mohamed,Shiba,Abou El-Regal,Khalil
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- A facile access to imidazo[2,1-b]thiazole and thiazolo[3,2-a]pyrimidine derivatives
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A new and efficient method for the synthesis of 2,3-dihydroimidazo [2,1-b]thiazoles 3, 2,3-dihydro-5H-thiazolo[3,2-a]pyrimidin-5-ones 4 and 2,3-dihydro-5H-thiazolo[3,2-a]pyrimidines 5 has been developed. The reactions of N′-(4,5-dihydrothiazol-2-yl)-N,N-dimethylamidines 1 with α-halogenoketones, acid chlorides or acrylic dienophiles were performed, leading to the title products.
- Landreau,Deniaud,Reliquet,Meslin
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p. 2015 - 2020
(2007/10/03)
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- Synthesis & Biological Activity of Some New Carboxamides, Carbohydrazides & Carbamates Derived from 2,3-Dihydro-5(H)-oxothiazolopyrimidine-6-carboxylic Acid
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Some new carboxamides (Va-j), carbohydrazides (Vk-p) and carbamates (VIIIa-d) derived from 2,3-dihydro-5(H)-oxothiazolopyrimidine-6-carboxylic acid (III) have been synthesised and evaluated for their antiinflammatory, antibacterial, antifungal and anthelmintic activities.The carboxamides (Ve,i,j) and carbohydrazides (Vk,n,o) possess promising antiinflammatory activity against carrageenin-induced paw oedema in rats, compound Ve being the most active member of the series showing 50.8 percent inhibition at 200 mg/kg (p.o.) dose.Ve, however, is found to be inactive at lower doses.None of the compounds shows any noteworthy antibacterial, antifungal or anthelmintic activities except Vk which displays promising antitubercular activity in vitro (MIC=5 mcg/ml) against Mycobacterium tuberculosis H37Rv.
- Shridhar, D. R.,Jogibhukta, M.,Joshi, P. P.,Rao, C. Seshagiri,Junnarkar, A. Y.
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p. 492 - 494
(2007/10/02)
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