902494-31-9

Usage

Uses

Used in Organic Synthesis:
TERT-BUTYL [1-(TRIFLUOROMETHYL)CYCLOPROPYL]CARBAMATE is used as a reagent in organic synthesis for its stability and protective properties towards other functional groups during reactions.
Used in Medicinal Chemistry:
In the pharmaceutical industry, TERT-BUTYL [1-(TRIFLUOROMETHYL)CYCLOPROPYL]CARBAMATE is used as a building block for the development of new drugs, leveraging its increased lipophilicity and electron-withdrawing properties to enhance drug efficacy and pharmacokinetics.
Used in Drug Design:
TERT-BUTYL [1-(TRIFLUOROMETHYL)CYCLOPROPYL]CARBAMATE is utilized in drug design for its unique geometric constraints provided by the cyclopropyl ring, which can influence the reactivity and selectivity of reactions, potentially leading to the creation of more effective and selective pharmaceutical agents.

InChI:InChI=1/C9H14F3NO2/c1-7(2,3)15-6(14)13-8(4-5-8)9(10,11)12/h4-5H2,1-3H3,(H,13,14)

Upstream product

• 277756-46-4 1-(trifluoromethyl)cyclopropanecarboxylic acid 
• 75-65-0 tert-butyl alcohol 
• 24424-99-5 di-tert-butyl dicarbonate 

Relevant academic research and scientific papers

THYROID HORMONE RECEPTOR BETA AGONIST COMPOUNDS

Provided herein are compounds, preferably thyroid hormone receptor beta (THR beta) agonist compounds, compositions thereof, and methods of their preparation, and methods of agonizing THR beta and methods for treating disorders mediated by THR beta.

TYROSINE KINASE INHIBITOR AND PHARMACEUTICAL COMPOSITION COMPRISING SAME

The present invention relates to a tyrosine kinase inhibitor and a pharmaceutical composition comprising same. The tyrosine kinase inhibitor of the present invention has the structures as shown in the following formula (I) or (II):

Discovery of APD371: Identification of a Highly Potent and Selective CB2 Agonist for the Treatment of Chronic Pain

The discovery of a novel, selective and fully efficacious CB2 agonist with satisfactory pharmacokinetic and pharmaceutical properties is described. Compound 6 was efficacious in a rat model of osteoarthritis pain following oral administration and, in contrast to morphine, maintained its analgesic effect throughout a 5-day subchronic treatment paradigm. These data were consistent with our hypothesis that full agonist efficacy is required for efficient internalization and recycling of the CB2 receptor to avoid tachyphylaxis. Based on its overall favorable preclinical profile, 6 (APD371) was selected for further development for the treatment of pain.

Discovery of novel HCV inhibitors: Synthesis and biological activity of 6-(indol-2-yl)pyridine-3-sulfonamides targeting hepatitis C virus NS4B

A novel series of 6-(indol-2-yl)pyridine-3-sulfonamides was prepared and evaluated for their ability to inhibit HCV RNA replication in the HCV replicon cell culture assay. Preliminary optimization of this series furnished compounds with low nanomolar potency against the HCV genotype 1b replicon. Among these, compound 8c has identified as a potent HCV replicon inhibitor (EC50 = 4 nM) with a selectivity index with respect to cellular GAPDH of more than 2500. Further, compound 8c had a good pharmacokinetic profile in rats with an IV half-life of 6 h and oral bioavailability (F) of 62%. Selection of HCV replicon resistance identified an amino acid substitution in HCV NS4B that confers resistance to these compounds. These compounds hold promise as a new chemotype with anti-HCV activity mediated through an underexploited viral target.

SUBSTITUTED PYRAZOLO[1,5-a]PYRIMIDINE COMPOUNDS AS TRK KINASE INHIBITORS

Compounds of Formula (I) and salts thereof in which R1, R2, R3, R4, X, Y and n have the meanings given in the specification, are inhibitors of Trk kinases and are useful in the treatment of diseases which can be treated with a Trk kinase inhibitor such as pain, cancer, inflammation, neurodegenerative diseases and certain infectious diseases.

Optimization of pharmacokinetics through manipulation of physicochemical properties in a series of HCV inhibitors

A novel series of HCV replication inhibitors based on a pyrido[3,2-d]pyrimidine core were optimized for pharmacokinetics (PK) in rats. Several associations between physicochemical properties and PK were identified and exploited to guide the design of comp

2,4,6-TRISUBSTITUTED PYRIDO (3,2-d) PYRIMIDINES USEFUL FOR TREATING VIRAL INFECTIONS

Pyrido(3,2-d)pyrimidine derivatives represented by the structural formuia (Ia): wherein, R1, R2 and R3 are defined herein, pharmaceutical acceptable addition salts, stereochemical isomeric forms, N-oxides, solvates and pro

Synthesis and structure-activity relationship of 1,2,4-triazole-containing diarylpyrazolyl carboxamide as CB1 cannabinoid receptor-ligand

Numerous research groups have been engaged in searching for novel CB1 receptor antagonists, since SR141716A (rimonabant), a CB1 receptor antagonist, proved to be efficacious in human for the treatment of obesity. In the present study, a series of 1,2,4-triazole-containing diarylpyrazolyl carboxamides based on the 1,5-diarylpyrazole template of rimonabant, was synthesized and tested for CB1 receptor binding affinity. The structure-activity relationship studies demonstrated that incorporation of 1,2,4-triazole ring onto the pyrazole scaffold via a methylene linker led to a significant improvement for CB1 receptor binding affinity. Importantly, these analogues also exhibited excellent selectivity for CB1 receptor over CB2 receptor.

New 3-alkylamino-4H-thieno-1,2,4-thiadiazine 1,1-dioxide derivatives activate ATP-sensitive potassium channels of pancreatic beta cells

Compound 1a (NN414) is a potent opener of Kir6.2/SUR1 KATP channels. Compound 1a inhibits insulin release in vitro and in vivo and preserves beta cell function in preclinical animal models suggesting that such a compound could find use in treatment or prevention of type 1 and type 2 diabetes. The crystal structure and a convergent synthesis of 1a are presented together with a range of new analogues of 1a. Several compounds, e.g., 6-chloro-3-(1-methyl-1-phenylethyl)amino-1H-thieno[3,2-e]-1,2,4-thiadiazine 1,1-dioxide (1h), were found to be potent openers of Kir6.2/SUR1 KATP channels and were able to suppress glucose-stimulated insulin release from rat islets in vitro (EC50 = 0.04 ± 0.01 μM) and in vivo after intravenous or peroral administration to hyperinsulinemic obese Zucker rats (ED50 = 4.0 mg/kg). Structural modifications of this series of K ATP channel openers have provided compounds with promising pharmaco-kinetic properties indicating that brief periods of beta cell rest can be achieved.