Category: 933785-18-3

Meyers, Marvin J. et al. published their research in Journal of Medicinal Chemistry in 2010 | CAS: 933785-18-3

Methyl 4-bromo-2-(trifluoromethoxy)benzoate (cas: 933785-18-3) belongs to organobromine compounds. Most of the natural organobromine compounds are produced by marine organisms, and several brominated metabolites with antibacterial, antitumor, antiviral, and antifungal activity have been isolated from seaweed, sponges, corals, molluscs, and others. Commercially available organobromine pharmaceuticals include the vasodilator nicergoline, the sedative brotizolam, the anticancer agent pipobroman, and the antiseptic merbromin. Synthetic Route of C9H6BrF3O3

Discovery of (3S,3aR)-2-(3-Chloro-4-cyanophenyl)-3-cyclopentyl-3,3a,4,5-tetrahydro-2H-benzo[g]indazole-7-carboxylic Acid (PF-3882845), an Orally Efficacious Mineralocorticoid Receptor (MR) Antagonist for Hypertension and Nephropathy was written by Meyers, Marvin J.;Arhancet, Graciela B.;Hockerman, Susan L.;Chen, Xiangyang;Long, Scott A.;Mahoney, Matthew W.;Rico, Joseph R.;Garland, Danny J.;Blinn, James. R.;Collins, Joe T.;Yang, Shengtian;Huang, Horng-Chih;McGee, Kevin F.;Wendling, Jay M.;Dietz, Jessica D.;Payne, Maria A.;Homer, Bruce L.;Heron, Marcia I.;Reitz, David B.;Hu, Xiao. And the article was included in Journal of Medicinal Chemistry in 2010.Synthetic Route of C9H6BrF3O3 This article mentions the following:

We have discovered a novel class of nonsteroidal pyrazoline antagonists of the mineralocorticoid receptor (MR) that show excellent potency and selectivity against other nuclear receptors. Early analogs were poorly soluble and had a propensity to inhibit the hERG channel. Remarkably, both of these challenges were overcome by incorporation of a single carboxylate moiety. Structural modification of carboxylate-containing lead R-4g with a wide range of substituents at each position of the pyrazoline ring resulted in R-12o, which shows excellent activity against MR and reasonable pharmacokinetic profile. Introduction of conformational restriction led to a novel series characterized by exquisite potency and favorable steroid receptor selectivity and pharmacokinetic profile. Oral dosing of 3S,3aR-27d (PF-3882845) in the Dahl salt sensitive preclin. model of salt-induced hypertension and nephropathy showed blood pressure attenuation significantly greater than that with eplerenone, reduction in urinary albumin, and renal protection. As a result of these findings, 3S,3aR-27d was advanced to clin. studies. In the experiment, the researchers used many compounds, for example, Methyl 4-bromo-2-(trifluoromethoxy)benzoate (cas: 933785-18-3Synthetic Route of C9H6BrF3O3).

Methyl 4-bromo-2-(trifluoromethoxy)benzoate (cas: 933785-18-3) belongs to organobromine compounds. Most of the natural organobromine compounds are produced by marine organisms, and several brominated metabolites with antibacterial, antitumor, antiviral, and antifungal activity have been isolated from seaweed, sponges, corals, molluscs, and others. Commercially available organobromine pharmaceuticals include the vasodilator nicergoline, the sedative brotizolam, the anticancer agent pipobroman, and the antiseptic merbromin. Synthetic Route of C9H6BrF3O3

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Meyers, Marvin J. et al. published their research in Journal of Medicinal Chemistry in 2010 | CAS: 933785-18-3

Methyl 4-bromo-2-(trifluoromethoxy)benzoate (cas: 933785-18-3) belongs to organobromine compounds. Most of the natural organobromine compounds are produced by marine organisms, and several brominated metabolites with antibacterial, antitumor, antiviral, and antifungal activity have been isolated from seaweed, sponges, corals, molluscs, and others. Commercially available organobromine pharmaceuticals include the vasodilator nicergoline, the sedative brotizolam, the anticancer agent pipobroman, and the antiseptic merbromin. Synthetic Route of C9H6BrF3O3

Discovery of (3S,3aR)-2-(3-Chloro-4-cyanophenyl)-3-cyclopentyl-3,3a,4,5-tetrahydro-2H-benzo[g]indazole-7-carboxylic Acid (PF-3882845), an Orally Efficacious Mineralocorticoid Receptor (MR) Antagonist for Hypertension and Nephropathy was written by Meyers, Marvin J.;Arhancet, Graciela B.;Hockerman, Susan L.;Chen, Xiangyang;Long, Scott A.;Mahoney, Matthew W.;Rico, Joseph R.;Garland, Danny J.;Blinn, James. R.;Collins, Joe T.;Yang, Shengtian;Huang, Horng-Chih;McGee, Kevin F.;Wendling, Jay M.;Dietz, Jessica D.;Payne, Maria A.;Homer, Bruce L.;Heron, Marcia I.;Reitz, David B.;Hu, Xiao. And the article was included in Journal of Medicinal Chemistry in 2010.Synthetic Route of C9H6BrF3O3 This article mentions the following:

We have discovered a novel class of nonsteroidal pyrazoline antagonists of the mineralocorticoid receptor (MR) that show excellent potency and selectivity against other nuclear receptors. Early analogs were poorly soluble and had a propensity to inhibit the hERG channel. Remarkably, both of these challenges were overcome by incorporation of a single carboxylate moiety. Structural modification of carboxylate-containing lead R-4g with a wide range of substituents at each position of the pyrazoline ring resulted in R-12o, which shows excellent activity against MR and reasonable pharmacokinetic profile. Introduction of conformational restriction led to a novel series characterized by exquisite potency and favorable steroid receptor selectivity and pharmacokinetic profile. Oral dosing of 3S,3aR-27d (PF-3882845) in the Dahl salt sensitive preclin. model of salt-induced hypertension and nephropathy showed blood pressure attenuation significantly greater than that with eplerenone, reduction in urinary albumin, and renal protection. As a result of these findings, 3S,3aR-27d was advanced to clin. studies. In the experiment, the researchers used many compounds, for example, Methyl 4-bromo-2-(trifluoromethoxy)benzoate (cas: 933785-18-3Synthetic Route of C9H6BrF3O3).

Methyl 4-bromo-2-(trifluoromethoxy)benzoate (cas: 933785-18-3) belongs to organobromine compounds. Most of the natural organobromine compounds are produced by marine organisms, and several brominated metabolites with antibacterial, antitumor, antiviral, and antifungal activity have been isolated from seaweed, sponges, corals, molluscs, and others. Commercially available organobromine pharmaceuticals include the vasodilator nicergoline, the sedative brotizolam, the anticancer agent pipobroman, and the antiseptic merbromin. Synthetic Route of C9H6BrF3O3

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary