Silica Sulfuric Acid: An Efficient and Reusable Catalyst for the One‐Pot Synthesis of 3,4‐Dihydropyrimidin‐2(1H)‐ones.

Abstract

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Synthesis of N-alkyl (aril)-tetra pyrimidine thiones and investigation of their human carbonic anhydrase I and II inhibitory effects

“…hCA II, the dominant physiologic isoform 90,91 , was potently inhibited by all newly synthesised N-alkyl (aril)-tetra pyrimidine thiones (1-5) with K i s in the range of 181.8 ± 41.9-273.6 ± 41.4 p.m. Also, similar to hCA I, the most powerful hCA II inhibition property was shown by allyl 6-methyl-2-thioxo-4-(p-tolyl)-1,2,3,4-tetrahydropyrimidine-5-carboxylate (1) with K i value of 155.4 ± 25.9 p.m. Also, AZA, which was used as clinical CA inhibitor, showed a K i value of 271.8 ± 54.5 p.m. This result clearly showed that all newly synthesised N-alkyl (aril)-tetra pyrimidine thiones (1)(2)(3)(4)(5) .…”

“…Many types of CAIs have been reported recently, together with their potential applications 27,28 . Some newly synthesised N-alkyl (aril)-tetra pyrimidine thiones (1)(2)(3)(4)(5) were screened for the inhibition of both human CA isoforms involved in important physiologic or pathologic processes, i.e. the cytosolic, hCA I, and II.…”

“…The search of physiologically active compounds with various applications expanded exponentially in the last period in the search of drugs with better efficacy and less side effects [1][2][3][4] . The pyrimidine-thiones possess relevant pharmacological activity, and the development of optimal synthetic methods for some of their classes is of interest 5 .…”

A One-pot Multi-component Synthesis of Dihydropyrimidinone/Thione and Dihydropyridine Derivatives via Biginelli and Hantzsch Condensations using t-BuOK as a Catalyst Under Solvent-free Conditions

“…The use of BF 3 .OEt 2 [44], polyphosphate ester [45], (NH 4 ) 2 CO 3 [46], NaCl [47] and {Fe 2 CuO} clusters [48] has also been described. The Biginelli reaction can strongly be accelerated by various procedures including heteropoly acids [49], silica sulfuric acid [50] and ferric chloride/tetraethyl orthosilicate [51].…”

Rapid preparation of the mitotic kinesin Eg5 inhibitor monastrol using controlled microwave-assisted synthesis

“…For this particular Biginelli 25 as promoters for this Biginelli reaction. While in the original Biginelli protocol EtOH was used as protic solvent 10,13,23 , suitable alternative solvents are MeCN 16,18,[20][21]25 and tetrahydrofuran (THF) 14 . With respect to environment-friendly procedures, several groups have developed solvent-free synthesis of monastrol 3,15,17,19,22,24 .…”