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2018•Radiochimica ActaRequires access

Synthesis of isotope – labeled selective PDE5 inhibitor sildenafil (UK 92480-10)

R. Sekhar Bolla, Kali Charan Gulipalli, N. Murthy Gandikota, Srinu Bodige, I. V. Kasi Viswanath

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Abstract

Abstract Sildenfil a vasodilating agent is a selective inhibitor of cyclic guanosine monophosphate – specific phosphodiesterase type 5 which is used for the treatment of male erectile dysfunction and pulmonary arterial hypertension. We presented a detailed approach for the synthesis of [2H3]sildenafil, [2H8]sildenafil and N-desmethyl [2H8]sildenafil. By using the approach we successfully synthesized [2H3]sildenafil, [2H8]sildenafil and N-desmethyl [2H8]sildenafil with good isotopic abundance.

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What this paper is about

Abstract Sildenfil a vasodilating agent is a selective inhibitor of cyclic guanosine monophosphate – specific phosphodiesterase type 5 which is used for the treatment of male erectile dysfunction and pulmonary arterial hypertension. We presented a detailed approach for the synthesis of [2H3]sildenafil, [2H8]sildenafil and N-desmethyl [2H8]sildenafil. By using the approach we successfully synthesized [2H3]sildenafil, [2H8]sildenafil and N-desmethyl [2H8]sildenafil with good isotopic abundance.

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Available abstract

Abstract Sildenfil a vasodilating agent is a selective inhibitor of cyclic guanosine monophosphate – specific phosphodiesterase type 5 which is used for the treatment of male erectile dysfunction and pulmonary arterial hypertension. We presented a detailed approach for the synthesis of [2H3]sildenafil, [2H8]sildenafil and N-desmethyl [2H8]sildenafil. By using the approach we successfully synthesized [2H3]sildenafil, [2H8]sildenafil and N-desmethyl [2H8]sildenafil with good isotopic abundance.

Key concepts: Sildenafil, Chemistry, Cyclic guanosine monophosphate, cGMP-specific phosphodiesterase type 5, Erectile dysfunction, Vasodilation, Pharmacology, Guanosine

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