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A Facile Synthesis of Raltegravir Potassium—An HIV Integrase Inhibitor
Author(s) -
Karumanchi Kishore,
Nangi Gangadhara Bhima Shankar,
Danda Subba Reddy,
Chavakula Ramadas,
Korupolu Raghu Babu,
Bonige Kishore Babu
Publication year - 2019
Publication title -
journal of heterocyclic chemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.321
H-Index - 59
eISSN - 1943-5193
pISSN - 0022-152X
DOI - 10.1002/jhet.3663
Subject(s) - raltegravir , chemistry , integrase , integrase inhibitor , potassium , reagent , combinatorial chemistry , amine gas treating , hydrochloride , human immunodeficiency virus (hiv) , organic chemistry , biochemistry , antiretroviral therapy , virology , viral load , gene , biology
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.