Journal ArticleDOI
Routes to Pyrazolo[3,4‐e][1,4]thiazepine, Pyrazolo[1,5‐a]pyrimidine and Pyrazole Derivatives
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TLDR
In this paper, Aminopyrazole was condensed with aryl aldehydes to give the 4-arylidenes derivative and Diazotized with resorcinol to give pyrazole derivative 5a.Abstract:
5-Aminopyrazole 1 was condensed with aryl aldehydes to give the 4-arylidenes 2. Compound 2 reacted with thioglycolic acid and ethyl cyanoacetate to give the pyrazolothiazepines 3 and pyrazolopyrimidines 4, respectively. Diazotized 2a coupled with resorcinol to give the pyrazole derivative 5a. Reaction of 1a with β-keto esters 7, 8 and acetoacetanilides 13 afforded the pyrazolopyrimidines 11, 12 and 15, respectively. Condensation of 1a with 2-acetylindan-1,3-dione 16 yielded fused pyrazolopyrimidine 18. Compound 1a also reacted with the enaminonitriles 19 and 22 to give the pyrazolopyrimidine 20 and 24, respectively.read more
Citations
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Journal ArticleDOI
An insight on synthetic and medicinal aspects of pyrazolo[1,5-a]pyrimidine scaffold
Srinivasulu Cherukupalli,Rajshekhar Karpoormath,Balakumar Chandrasekaran,Girish A. Hampannavar,Neeta Thapliyal,Venkata Narayana Palakollu +5 more
TL;DR: Current review is the first attempt made towards the compilation of significant advances made on pyrazolo[1,5-a]pyrimidines reported since 1980s and extensively reveals significant biological properties along with SAR studies.
Journal ArticleDOI
New trends in the chemistry of 5‐aminopyrazoles
Journal ArticleDOI
5-Amino-pyrazoles: potent reagents in organic and medicinal synthesis
TL;DR: 5-Amino-pyrazoles represent a class of promising functional reagents, similar to the biologically active compounds, highlighted with diverse applications especially in the field of pharmaceutics and medicinal chemistry.
Journal ArticleDOI
Efficient one-pot synthesis of spiro[indoline-3,4'-pyrazolo[3,4-e][1,4]thiazepine] dione via three-component reaction
Hui Chen,Daqing Shi +1 more
TL;DR: An efficient one-pot synthesis of spiro[indoline-3,4′-pyrazolo] dione derivatives via three-component reaction of 5-amino-3-methylpyrazole, isatin, and thioacid is described in this article.
Patent
Bicyclic pyrimidines as dipeptidyl peptidase-iv inhibitors for the treatment or prevention of diabetes
TL;DR: In this paper, substituted bicyclic pyrimidines are used as inhibitors of the dipeptidyl peptidase-IV enzyme (DPP-IV inhibitors) and which are useful in the treatment or prevention of diseases, such as diabetes and particularly Type 2 diabetes.
References
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Journal ArticleDOI
Synthesis and antischistosomal activity of certain pyrazolo[1,5-a]pyrimidines.
Keitaro Senga,Thomas Novinson,Robert H. Springer,Ravindra Pralap Rao,D. E. O'brien,Roland K. Robins,Henry R. Wilson +6 more
TL;DR: None of the compounds exhibiting in vitro activity were active against S. mansoni in vivo, and the greatest degree of activity in vitro was found with the 7-mercaptopyrazolo[1,5-a]pyrimidines.
Journal ArticleDOI
Thiazolinone analogs of indolmycin with antiviral and antibacterial activity
TL;DR: 2-monoalkylaminothiazolinone analogues have in vitro activity against both RNA viruses and bacteria and only the levorotatory enantiomer 46, with the same absolute stereochemistry as natural indolmycin, has antimicrobial activity.
Journal ArticleDOI
Synthesis of Substituted Azaindenes: Synthesis of New Pyrazolo[1,5-a]pyrimidine Derivatives
TL;DR: Several pyrazolo[1,5-a]pyrimidines were synthesized via the reaction of 4,5disubstituted 3-aminopyrazoles 1a-d with 3-dimethylaminopropiophenone, cinnamaldehyde, benzylideneacetophenone and tetracyanoethylene as mentioned in this paper.
Journal ArticleDOI
Nitriles in heterocyclic synthesis: Synthesis of pyrazolo[1, 5‐a] pyrimidine, pyrazolo[1, 5‐c][1, 2, 4]triazine and pyrazolo[4, 3‐e][1, 2, 4]triazine derivatives
TL;DR: Amino-3-phenylpyrazole (1) reacted with enaminonitriles 2a-c to afford the pyrazolopyrimidines 5a, b and the 5substituted aminopyrazole 8. 5a reacted with arenediazonium chlorides and benzaldehyde to give 6 and 7 respectively as mentioned in this paper.
Journal ArticleDOI
Reaction of 5‐aminopyrazole derivatives with ethoxymethylene‐malononitrile and its analogues
Katsuhiko Nagahara,Hiroko Kawano,Shinji Sasaoka,Chisa Ukawa,Tamaki Hirama,Atsushi Takada,Howard B. Cottam,Roland K. Robins +7 more
TL;DR: In this article, a one-pot synthesis using 5-aminopyrazole derivatives with EMMN, ECA, or diethyl ethoxymethylenemalonate (DEMM) gave pyrazolo-[1,5-a]pyrimidine compounds.