535932-30-0Relevant academic research and scientific papers
Sulphonated graphene oxide catalyzed continuous flow synthesis of pyrazolo pyrimidinones, sildenafil and other PDE-5 inhibitors
Sthalam, Vinay Kumar,Mahajan, Bhushan,Karra, Purushotham Reddy,Singh, Ajay K.,Pabbaraja, Srihari
, p. 326 - 330 (2022/01/19)
Sulphonated graphene oxide was used for cascade condensation and cyclization reactions towards accessing substituted pyrazolo pyrimidinones. Further, sulphonation and amination reactions were integrated through continuous flow chemistry to access PDE-5 inhibitors. Herein, we report a simple continuous synthetic platform that reduce tedious manual operations and accelerate the synthesis of several potent inhibitors of phosphodiesterase type-5. The developed platform enabled us to perform one-flow multi-step, multi-operational process to synthesize the PDE-5 inhibitors such as sildenafil and its analogues in 32.3 min of the reaction time, with minimal human intervention and single solvent.
A highly efficient heterogeneous palladium-catalyzed carbonylative annulation of 2-aminobenzamides with aryl iodides leading to quinazolinones
You, Shengyong,Huang, Bin,Yan, Tao,Cai, Mingzhong
, p. 35 - 45 (2018/09/14)
The first heterogeneous carbonylative annulation of 2-aminobenzamides with aryl iodides was achieved in N,N-dimethylformamide (DMF) at 120 °C under 10 bar of carbon monoxide by using an MCM-41-immobilized bidentate phosphine palladium(II) complex [MCM-41-2P-Pd(OAc)2] as catalyst and 1,8-diazabicycloundec-7-ene (DBU) as base, yielding a wide variety of quinazolinone derivatives in good to excellent yields. The new heterogeneous palladium catalyst can easily be prepared by a simple procedure from commercially readily available reagents, and recovered by filtration of the reaction solution, and recycled up to eight times without significant loss of activity.
Novel bicyclic heterocyclic compounds, process for their preparation and compositions containing them
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Page/Page column 76, (2008/06/13)
The present invention provides, among other things, new bicyclo heterocyclic compounds, compositions comprising these heterocyclic compounds, methods of making the heterocyclic compounds, and methods of using these heterocyclic compounds for treating a variety of conditions and disease states associated with, for example, cellular proliferation, inflammation, glycosidase expression, or the low expression of Perlecan.
An efficient one-pot synthesis of pyrazolopyrimidines, intermediates for potential phosphodiesterase inhibitors
Abdel-Jalil, Raid J.,Khanfar, Monther,Abu-Safieh, Kayed,Al-Gharabli, Samer,El-Abadelah, Mustafa,Voelter, Wolfgang
, p. 619 - 624 (2007/10/03)
A simple high-yielding procedure is presented for the synthesis of pyrazolopyrimidinones overcoming limitations found in earlier work and of considerable utility for the production of intermediates for potential phosphodiesterase inhibitors. Springer-Verlag 2005.
High throughput synthesis of pyrazolopyrimidines via copper- catalysed cyclization and X-ray study
Abdel-Jalil, Raid J.,Khanfar, Monther,Al-Gharabli, Samer,El-Abadelah, Mustafa M.,Eichele, Klaus,Anwar, Muhammad Usman,Voelter, Wolfgang
, p. 1821 - 1827 (2007/10/03)
A rapid and easy high-yielding synthesis of pyrazolopyrimidinones in the presensce of copper chloride is described. To fully confirm the structure of a Viagra intermediate, the X-Ray structure of 5-(2-ethoxyphenyl)-1-methyl-3- propyl-1,6-dihydropyrazolo[4,3-d]pyrimidin-7-one (2a) was determined.
A facile synthesis of 5-arylpyrazolo[4,3-d]-pyrimidin-7-ones
Maruthikumar,Rao, P. Hanumantha
, p. 343 - 345 (2007/10/03)
A series of 1-methyl-3-propyl-6,7-dihydro-1H-pyrazolo[4,3-d]pyrimidin-7-ones substituted in the 5-position with various aryl substituents has been synthesized by the reaction of corresponding Schiff bases with 4-amino-1-methyl-3-propylpyrazole-5-carboxamide in the presence of acetic acid.
