A Facile Synthesis of Raltegravir Potassium—An HIV Integrase Inhibitor

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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Bibliographic Details
Published in:Journal of heterocyclic chemistry Vol. 56; no. 9; pp. 2683 - 2690
Main Authors: Karumanchi, Kishore, Nangi, Gangadhara Bhima Shankar, Danda, Subba Reddy, Chavakula, Ramadas, Korupolu, Raghu Babu, Bonige, Kishore Babu
Format: Journal Article
Language:English
Published: Hoboken Wiley Subscription Services, Inc 01-09-2019
Subjects:
Potassium
Reagents
Synthesis
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Description
Summary: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