Design, synthesis and biological evaluation of novel azaspiro analogs of linezolid as antibacterial and antitubercular agents was written by Gadekar, Pradip K.;Roychowdhury, Abhijit;Kharkar, Prashant S.;Khedkar, Vijay M.;Arkile, Manisha;Manek, Hardik;Sarkar, Dhiman;Sharma, Rajiv;Vijayakumar, V.;Sarveswari, S.. And the article was included in European Journal of Medicinal Chemistry in 2016.Application In Synthesis of 3-(Trifluoromethyl)benzene-1-sulfonyl chloride This article mentions the following:
The design, synthesis and antimicrobial evaluation of a novel series of azaspiro analogs I [R = acetyl, 4-(trifluoromethyl)benzoyl, nicotinoyl, etc.] of linezolid were described. Linezolid comprises of a morpholine ring which was known for its metabolism-related liabilities. Therefore, the key modification made in the linezolid structure was the replacement of morpholine moiety with its bioisostere, 2-oxa-6-azaspiro[3.3]heptane. Furthermore, the replacement of N-acetyl terminal of linezolid with various aromatic or aliphatic functionalities was carried out. The title compounds were evaluated against a panel of Gram-pos. and Gram-neg. bacteria and Mycobacterium tuberculosis. Subsequent structure-activity relationship (SAR) studies identified several compounds with mixed antibacterial and antitubercular profiles. Compound I [R = isoxazole-5-carbonyl] (IC50 0.72, 0.51, 0.88, 0.49 渭g/mL for Escherichia coli, Pseudomonas aeruginosa, Staphylococcus aureus, Bacillussubtilis, resp.) exhibited similar antibacterial profile as linezolid. The N-acetyl derivative I [R = acetyl] was similar to linezolid in antitubercular profile. The use of azaspiro substructure in the medicinal chem. of antibacterial and antitubercular agents was demonstrated. In the experiment, the researchers used many compounds, for example, 3-(Trifluoromethyl)benzene-1-sulfonyl chloride (cas: 777-44-6Application In Synthesis of 3-(Trifluoromethyl)benzene-1-sulfonyl chloride).
3-(Trifluoromethyl)benzene-1-sulfonyl chloride (cas: 777-44-6) 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.Application In Synthesis of 3-(Trifluoromethyl)benzene-1-sulfonyl chloride
Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics