The discovery of long-acting saligenin β2 adrenergic receptor agonists incorporating a urea group was written by Procopiou, Panayiotis A.;Barrett, Victoria J.;Ford, Alison J.;Looker, Brian E.;Lunniss, Gillian E.;Needham, Deborah;Smith, Claire E.;Somers, Graham. And the article was included in Bioorganic & Medicinal Chemistry in 2011.Synthetic Route of C7H7BrN2O2 This article mentions the following:
A series of novel, potent and selective human β2 adrenoceptor agonists incorporating a urea moiety on the terminal right-hand side Ph ring of (R)-salmeterol is presented. Urea 9j (I) had long duration of action in vitro on guinea pig trachea, and also in vivo similar to that of salmeterol. It had lower oral absorption and bioavailability than salmeterol in both rat and dog. It had a turnover ratio similar to salmeterol, with no evidence for formation of any aniline metabolites in human liver microsomes and hepatocytes. However no crystalline salts suitable for inhaled delivery were identified. In the experiment, the researchers used many compounds, for example, 2-Bromo-4-methyl-6-nitroaniline (cas: 827-24-7Synthetic Route of C7H7BrN2O2).
2-Bromo-4-methyl-6-nitroaniline (cas: 827-24-7) belongs to organobromine compounds. Many of the organo bromine compounds are relatively nonpolar. Bromine is more electronegative than carbon (2.8 vs 2.5) and hence the carbon in a carbonbromine bond is electrophilic in nature. Many of the alkyl bromine derivatives are excellent alkylating agents since bromides are good leaving groups. Tribromides, like tetrabutylammonium tribromide, are used as a solid source of bromine. N-bromosuccimide (NBS) is used for the selective bromination of allylic bonds.Synthetic Route of C7H7BrN2O2
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary