Synthesis and Anti-HIV-1 Evaluation of New Sonogashira-Modified Emivirine (MKC-442) Analogues was written by Danel, Krzysztof;Joergensen, Per T.;Pedersen, Erik B.;La Colla, Paolo;Collu, Gabriella;Loddo, Roberta. And the article was included in Helvetica Chimica Acta in 2009.Name: 2-(Chloromethyl)-1,3-difluorobenzene This article mentions the following:
The MKC-442 analog 6-(3,5-dimethylbenzyl)-5-ethyluracil substituted with a (propargyloxy)methyl group at N(1) has previously been found highly active against HIV-1. The CC bond in the substituent at N(1) is here utilized in a series of chem. reactions in order to develop new agents with higher activity against HIV-1-resistant mutants. The syntheses involved Pd-catalyzed C,C-coupling reactions, addition of disulfides, and click chem. on the terminal CC bond as well as addition of bromine to the so formed internal CC bonds. Sonogashira couplings were performed with silyl-derivatized iodobenzyl alcs. which, after deprotection, were oxidized to aldehydes by means of IBX. The isomeric alc. I was obtained in the Sonogashira reaction of propargyl alc. with the N(1)-substituted (4-iodobenzyloxy)methyl derivative of the above mentioned uracil. Compound I turned out to be the most effective compound against problematic HIV-1 mutants. The general observation in the present work is that a combination of alkyne and aryl in the substituent at N(1) leads to highly active compounds against HIV-1. In the experiment, the researchers used many compounds, for example, 2-(Chloromethyl)-1,3-difluorobenzene (cas: 697-73-4Name: 2-(Chloromethyl)-1,3-difluorobenzene).
2-(Chloromethyl)-1,3-difluorobenzene (cas: 697-73-4) belongs to organic chlorides. Organic chlorides can be used in production of: PVC, pesticides, chloromethane, teflon, insulators. Aryl chlorides may be prepared by the Friedel-Crafts halogenation, using chlorine and a Lewis acid catalyst.Name: 2-(Chloromethyl)-1,3-difluorobenzene
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