1357931-55-5Relevant articles and documents
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.
NOVEL DUAL MODE OF ACTION SOLUBLE GUANYLATE CYCLASE ACTIVATORS AND PHOSPHODIESTERASE INHIBITORS AND USES THEREOF
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Page/Page column 74, (2020/06/19)
The present invention relates to compounds of formula (I) or formula (II) or pharmaceutically acceptable salt, solvate or hydrate thereof, wherein said compound of formula (I) and said compound of formula II each comprises at least one ONO2 or ONO moiety; R1 is C1-C3alkyl; R2 is H, C1-C6alkyl, C3-C6cycloalkyl, C1-C2alkoxy, C2-C4alkenyl; R3 is C1-C4alkyl optionally substituted with C1-C2alkoxy, C3-C4cycloalkyl, C2-C4alkenyl; R4 and R5 are each independently H or C1-C6alkyl optionally substituted with F, OH, ONO, ONO2, COOH, C1-C3alkoxy, C3-C6cycloalkyl; or together with the nitrogen atom to which they are attached form a heterocyclic ring, wherein preferably said heterocyclic ring is selected from aziridine, azetidine, pyrollidine, piperidine, morpholine, piperazine, homo-piperazine, 2,5-diazabicyclo[2,2,1]heptane and 3,7-diazabicyclo[3,3,0]octane, wherein said heterocyclic ring is optionally substituted with independently one or more R6; R6 is C1-C6alkyl optionally substituted with independently one or more halogen, OH, ONO, ONO2, C1-C3alkoxy, C1-C3haloalkoxy, COOR7, NR8R9, C=NR10; R7 is H, or C1-C4alkyl optionally substituted with F, OH, ONO, ONO2, NR8R9; R8 and R9 are independently H, or C1-C4alkyl optionally substituted with ONO, ONO2; R10 is C1-C4alkyl optionally substituted with F, ONO, ONO2; C3-C6cycloalkyl; pharmaceutical compositions thereof, and their use in methods of treating or preventing a disease alleviated by inhibition of PDE5 in a human or in a non-human mammal.
A method for synthesis of impurity D Xidinafei (by machine translation)
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Paragraph 0059; 0060; 0061; 0062-0085, (2019/08/28)
The invention relates to a method for synthesis of impurity D Xidinafei, sulfuryl Xidinafei body chlorine to as raw material in the middle, the middle of the stated Xidinafei sulfurylbody chlorine in adding water and organic solvent, heating to reflux for
Liquid-chromatography determination of impurities in sildenafil citrate
Kumar, A.Phani,Ganesh,Prasad, K. Hari,Hariharakrishnan,Dubey,Rao, B. Venugopala
experimental part, p. 1219 - 1222 (2012/01/05)
A simple, economic and time-efficient stability-indicating, reversed phase liquid chromatographic (RP-LC) method has been developed for the analysis of sildenafil citrate in the presence of both process related impurities and degradation products generated by decomposition. The drug was subjected to stress conditions of hydrolysis, oxidation, photolysis and thermal degradation. Considerable degradation was found to occur in alkali and oxidative stress conditions. The drug was found to be stable to other stress conditions attempted. The stress samples were assayed against a qualified reference standard and the mass balance was found close to 99.6 %. The method was validated with respect to specificity, linearity, accuracy, precision, robustness, limit of detection and quantification. The method is simple, rapid, selective, accurate and stability indicating, useful in the quality control of bulk manufacturing of sildenafil.