Tag: 152.08

Park, No Sang et al. published their research in Yakhak Hoechi in 1990 | CAS: 108655-63-6

3-(Trifluoromethyl)isoxazol-5-amine (cas: 108655-63-6) belongs to isoxazole derivatives. Isoxazoles present in various natural products and synthetic compounds of biological importance like antibacterial, antagonists, antiinflammatory, analgesics, and also show the applications in functional materials. The electrophilic cyclization of various 2-alkynone O-methyl oximes with a wide range of substrates such as ICl, I2, Br2, PhSeBr, etc. provides a variety of 3,4,5-trisubstituted isoxazoles in good to excellent yields.Application In Synthesis of 3-(Trifluoromethyl)isoxazol-5-amine

Development of antiinflammatory agents. I. Isoxazole derivatives was written by Park, No Sang;Kim, Hyun Sook;Min, Changhee;Choi, Joong Kwon. And the article was included in Yakhak Hoechi in 1990.Application In Synthesis of 3-(Trifluoromethyl)isoxazol-5-amine This article mentions the following:

3-Substituted 5-aminoisoxazole-4-carboxylates I (R = CF3, CHF2, Ph, 4-MeOC6H4, 2-, 3-, or 4-R1C6H4; R1 = F, Cl, CF3, NO2; R2 = Me) were prepared by the reaction of corresponding bromoaldoximes with cyanoacetate. I (R = CF3, R2 = Me) (II) was acylated with various aminopyridine derivatives to afford diamides. The ester group of II was hydrolyzed and decarboxylated easily to give 3-trifluoromethyl-5-aminoisoxazole. The aminoisooxazole was also converted to amides. The synthesized compounds were tested for antiinflammatory activities. In the experiment, the researchers used many compounds, for example, 3-(Trifluoromethyl)isoxazol-5-amine (cas: 108655-63-6Application In Synthesis of 3-(Trifluoromethyl)isoxazol-5-amine).

3-(Trifluoromethyl)isoxazol-5-amine (cas: 108655-63-6) belongs to isoxazole derivatives. Isoxazoles present in various natural products and synthetic compounds of biological importance like antibacterial, antagonists, antiinflammatory, analgesics, and also show the applications in functional materials. The electrophilic cyclization of various 2-alkynone O-methyl oximes with a wide range of substrates such as ICl, I2, Br2, PhSeBr, etc. provides a variety of 3,4,5-trisubstituted isoxazoles in good to excellent yields.Application In Synthesis of 3-(Trifluoromethyl)isoxazol-5-amine

Referemce:
Isoxazole – Wikipedia,
Isoxazole | C3H3NO – PubChem

Rowbottom, Martin W. et al. published their research in Journal of Medicinal Chemistry in 2012 | CAS: 108655-63-6

3-(Trifluoromethyl)isoxazol-5-amine (cas: 108655-63-6) belongs to isoxazole derivatives. Isoxazole are described as inhibitors of acetylcholinesterase (AChE). Isoxazole ligands bind to and inhibit the Sxc- antiporter. The most common methods for N–O bond cleavage in isoxazoles are hydrogenation with palladium or platinum catalysts or with Raney Ni. Recent developments have shown that Mo(CO)6 efficiently cleaves the N–O bond in isoxazoles.COA of Formula: C4H3F3N2O

Identification of 1-(3-(6,7-Dimethoxyquinazolin-4-yloxy)phenyl)-3-(5-(1,1,1-trifluoro-2-methylpropan-2-yl)isoxazol-3-yl)urea Hydrochloride (CEP-32496), a Highly Potent and Orally Efficacious Inhibitor of V-RAF Murine Sarcoma Viral Oncogene Homologue B1 (BRAF) V600E was written by Rowbottom, Martin W.;Faraoni, Raffaella;Chao, Qi;Campbell, Brian T.;Lai, Andiliy G.;Setti, Eduardo;Ezawa, Maiko;Sprankle, Kelly G.;Abraham, Sunny;Tran, Lan;Struss, Brian;Gibney, Michael;Armstrong, Robert C.;Gunawardane, Ruwanthi N.;Nepomuceno, Ronald R.;Valenta, Ianina;Hua, Helen;Gardner, Michael F.;Cramer, Merryl D.;Gitnick, Dana;Insko, Darren E.;Apuy, Julius L.;Jones-Bolin, Susan;Ghose, Arup K.;Herbertz, Torsten;Ator, Mark A.;Dorsey, Bruce D.;Ruggeri, Bruce;Williams, Michael;Bhagwat, Shripad;James, Joyce;Holladay, Mark W.. And the article was included in Journal of Medicinal Chemistry in 2012.COA of Formula: C4H3F3N2O This article mentions the following:

The Ras/RAF/MEK/ERK mitogen-activated protein kinase (MAPK) signaling pathway plays a central role in the regulation of cell growth, differentiation, and survival. Expression of mutant BRAFV600E results in constitutive activation of the MAPK pathway, which can lead to uncontrolled cellular growth. Herein, we describe an SAR optimization campaign around a series of quinazoline derived BRAFV600E inhibitors. In particular, the bioisosteric replacement of a metabolically sensitive tert-Bu group with fluorinated alkyl moieties is described. This effort led directly to the identification of a clin. candidate 1-(3-(6,7-dimethoxyquinazolin-4-yloxy)phenyl)-3-(5-(1,1,1-trifluoro-2-methylpropan-2-yl)isoxazol-3-yl)urea hydrochloride (CEP-32496, I). CEP-32496 exhibits high potency against several BRAFV600E-dependent cell lines and selective cytotoxicity for tumor cell lines expressing mutant BRAFV600E vs. those containing wild-type BRAF. It also exhibits an excellent PK profile across multiple preclin. species. In addition, significant oral efficacy was observed in a 14-day BRAFV600E-dependent human Colo-205 tumor xenograft mouse model, upon dosing at 30 and 100 mg/kg BID. In the experiment, the researchers used many compounds, for example, 3-(Trifluoromethyl)isoxazol-5-amine (cas: 108655-63-6COA of Formula: C4H3F3N2O).

3-(Trifluoromethyl)isoxazol-5-amine (cas: 108655-63-6) belongs to isoxazole derivatives. Isoxazole are described as inhibitors of acetylcholinesterase (AChE). Isoxazole ligands bind to and inhibit the Sxc- antiporter. The most common methods for N–O bond cleavage in isoxazoles are hydrogenation with palladium or platinum catalysts or with Raney Ni. Recent developments have shown that Mo(CO)6 efficiently cleaves the N–O bond in isoxazoles.COA of Formula: C4H3F3N2O

Referemce:
Isoxazole – Wikipedia,
Isoxazole | C3H3NO – PubChem