A Facile Synthesis of Raltegravir Potassium—An HIV Integrase Inhibitor

A facile, cost‐effective, and commercially viable synthesis of Raltegravir Potassium (1) has been developed from 2‐(1‐amino‐1‐methyl‐ethyl)‐N‐[(4‐fluorophenyl)methyl]‐1,6‐dihydro‐5‐hydroxy‐1‐methyl‐6‐oxo‐4‐pyrimidinecarboxamide (9) with high purity and in good yields. In addition, a new approach for...

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Veröffentlicht in:Journal of heterocyclic chemistry 2019-09, Vol.56 (9), p.2683-2690
Hauptverfasser: Karumanchi, Kishore, Nangi, Gangadhara Bhima Shankar, Danda, Subba Reddy, Chavakula, Ramadas, Korupolu, Raghu Babu, Bonige, Kishore Babu
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Sprache:eng
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Zusammenfassung:A facile, cost‐effective, and commercially viable synthesis of Raltegravir Potassium (1) has been developed from 2‐(1‐amino‐1‐methyl‐ethyl)‐N‐[(4‐fluorophenyl)methyl]‐1,6‐dihydro‐5‐hydroxy‐1‐methyl‐6‐oxo‐4‐pyrimidinecarboxamide (9) with high purity and in good yields. In addition, a new approach for the synthesis of key amine intermediate (9) of Raltegravir Potassium (1) from commercially available 2‐amino‐2‐methylpropanenitrile hydrochloride (2) is also described. The key features of the synthesis are fewer synthetic steps, employing the inexpensive reagents and eco‐friendly.
ISSN:0022-152X
1943-5193
DOI:10.1002/jhet.3663