GSK-2838232

New Drug Approvals

STR1

Figure imgf000135_0002

GSK-2838232

4-(((3aR,5aR,5bR,7aR,9S,11aR,11bR,13aS)-3a-((R)-2-((3-chlorobenzyl)(2-(dimethylamino)ethyl)amino)-1-hydroxyethyl)-1-isopropyl-5a,5b,8,8,11a-pentamethyl-2-oxo-3,3a,4,5,5a,5b,6,7,7a,8,9,10,11,11a,11b,12,13,13a-octadecahydro-2H-cyclopenta[a]chrysen-9-yl)oxy)-2,2-dimethyl-4-oxobutanoic acid.

28-Norlup-18-en-21-one, 3-(3-carboxy-3-methyl-1-oxobutoxy)-17-[(1R)-2-[[(4-chlorophenyl)methyl][2-(dimethylamino)ethyl]amino]-1-hydroxyethyl]-, (3β)-

Phase I

Glaxosmithkline Llc INNOVATOR

Mark Andrew HATCHER, Brian Alvin Johns,Michael Tolar Martin, Elie Amine TABET, Jun Tang

A reverse transcriptase inhibitor potentially for the treatment of HIV infection.

GSK-2838232; GSK-8232; 2838232

CAS No. 1443460-91-0

C48H73ClN2O6,809.56

SYNTHESIS

PART 1

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PART2

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PART3

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PART 4

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AND UNWANTEDISOMER SHOWN BELOW

PART5

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GSK2838232 is a novel human immune virus (HIV) maturation inhibitor being developed for the treatment of chronic HIV infection. GSK2838232 is a betulin derivative

Human immunodeficiency virus type 1 (HIV-1 ) leads to the contraction of acquired immune deficiency disease (AIDS). The number of cases of HIV continues to rise, and currently over twenty-five million individuals worldwide suffer from the virus. Presently, long-term suppression of viral replication with antiretroviral drugs is the only option for treating HIV-1 infection. Indeed, the U.S. Food and Drug Administration has approved twenty-five drugs over six…

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