Synthesis of pyrazolo[1,5-c]pyrimidines from …

Chemistry of 1,2,4-Triazines (XXIV)──Synthesis of Pyrazolo-(5,4-e)-1,2,4-triazine Derivatives[J].

Synthesis of pyrazolo[3,4-b][1,4]diazepines and pyrazolo…

Various halomethyleniminium salts as novel Vilsmeier agents were synthesized from formamide or N-methylformamide with POCl3. Treatment of N-1-substituted-aminopyrazoles including N-1-phenyl-5-aminopyrazoles, N-1-(2-pyridinyl)-5-aminopyrazoles, and N-1-(2-quinolinyl)-5-aminopyrazoles with these agents gave the corresponding pyrazolo[3,4-d]pyrimidine, N-(1H-pyrazol-5-yl)formamide, or N-(1H-pyrazol-5-yl)formamidine. The reaction was different from the traditional Vilsmeier-type reaction and the plausible reactive pathways were proposed for the unexpected result.

Synthesis of pyrazolo[5,1-a]isoquinolines through …

T1 - Selective synthesis of pyrazolo[3,4-d]pyrimidine, N-(1H-pyrazol-5-yl) formamide, or N-(1H-pyrazol-5-yl)formamidine derivatives from N-1-substituted-5-aminopyrazoles with new Vilsmeier-type reagents

Objective: A new series of hybrid pyrazolo[3,4-d]pyrimidine scaffold with a heteroaryl moiety as pyrazole, oxadiazole, triazole or phthalimide moiety (14a-f, 16, 17, 19, 20) was synthesized and biologically evaluated for the cytotoxicity against human liver cancer cell line (HEPG-2), human breast cancer cell line (MCF-7) and human colon cancer cell line (HCT-116).


Synthesis of 4-Hydroxyl Pyrazolo[3,4-d]pyrimidines …

ABSTRACT: Novel 1- Phenyl 1-H-Pyrazolo[3,4-d]Pyrimidine Derivatives were synthesized from the key intermediate chloro derivative (1).The conversion of chloro derivative(1) into 1,2,4 triazoles, 1,3,4 thiadiazoles and thiazoles was accomplished with the intermediacy of the ester(2) and hydrazide (3). Moreover triazole ring was annelated to the pyrazolopyrmidine core in two step reaction involving reaction with acid hydrazides followed by intramolecular cyclization in boiling glacial acetic acid Majority of the synthesized compounds showed variable antimicrobial activity on the hand tricyclic compounds(9a-b) were deprived from any antimicrobial activity against the tested micro-organisms. The hydrazine carbothioamide derivative (4) and 1,3,4 thiadiazole derivative (6) showed antimicrobial activity against Streptococcus pneumoniae and Bacillis subtilis comparable to ampicillin and a moderate antifungal activity against Asp. Fumigates and C. alb.

A New Approach for the Synthesis of Some Pyrazolo | …

Pyrazolo derivatives have been the basis of numerous drugs and dyes used in industries, hitherto of its possessing analgesic and antipyretic properties in addition to its base unit exhibiting dyeing characteristics. No doubt, owing to their synthetic utility in many products, interest in developing a new procedure becomes enviable. Quite a large number of medicinal plants in Indian subcontinent contain heterocyclic components in roots, stem and shoot system. Also a good number of the Pyrazolo derivatives are found in seeds, for example water melon seeds found to contain Pyrazolo in the concentration range of 250-410 μg/l on a specific variety. As for the bio synthetic activity is concerned, most plants have properties relating to anti-inflammatory, diagnostic acid, antibacterial, hypoglycemic, sedative-hypnotic etc. Herein, this paper deals with the synthesis and characterization of Pyrazolo derivative namely pyrazolidino [3, 4-b] quinoline by IR and NMR techniques. The data reveals the modified mode of synthesis from an intermediate stage up to the finalized product pertaining to the structure identified base as Pyrazolo quinoline.

Synthesis of pyrazolo(4,3‐ d )oxazoles - DeepDyve

A series of new pyrazolo[3,4-]pyridines bearing various 1, 3, 5 or 1, 3, 7 pattern substitutions, were designed and synthesized. Some of them showed interesting inhibitory activity mainly against glycogen synthase kinase 3 (GSK3)α/β as well as against cdc2-like kinases 1 (CLK1) and dual-specificity tyrosine phosphorylation-regulated kinase 1A (DYRK1A), with good selectivity and remarkable structure–activity relationships (SARs), without being cytotoxic. Molecular simulations in correlation with biological data revealed the importance of the existence of 1-H as well as the absence of a bulky 7-substituent.

Synthesis of some pyrazolo(1,5‐ c )(1,3)benzoxazines …

A great number of GSK3 inhibitors have been reported in the literature and some of them were found to ameliorate cognitive impairments) and reduce the amount of Aβ, together with the tau hyperphosphorylation in neuronal cells.) Although a number of putative allosteric inhibitors appeared in the literature,) most of the reported GSK3 inhibitors are ATP competitive, and are often characterized by the presense of a central purine-like heterocyclic scaffold, substituted with a characteristic carboxamide residue.,) Within this context and as part of a research program aimed to study modified purine analogues as potential protein kinase inhibitors, we have explored the pyrazolopyridine scaffold and present in this study the design, synthesis and evaluation of a number of new substituted pyrazolo[3,4-]pyridines for inhibitory potency against a panel of eight protein kinases.