84403-51-0

Upstream product

• 32122-11-5 4-benzyloxy-benzoic acid methyl ester 
• 74-89-5 methylamine 
• 1486-50-6 4-(benzyloxy)benzoic acid chloride 
• 593-51-1 methylamine hydrochloride 
• 1486-51-7 p-(benzyloxy)benzoic acid 

Downstream Products

• 1258001-38-5 5-(4-(benzyloxy)phenyl)-1-methyl-1H-tetrazole 
• 380243-70-9 4-(1-methyl-1H-tetrazol-5-yl)phenol 

Relevant academic research and scientific papers

Silver-Mediated N-Trifluoromethylation of Amides and Peptides

We report herein the direct N-trifluoromethylation of N-H amides. Promoted by AgOTf and 2-fluoropyridine, the reaction of a variety of amides with Selectfluor, TMSCF3 and CsF proceeds smoothly at room temperature leading to the corresponding N-trifluoromethylated products in satisfactory yields. The protocol is also applicable to amino acid derivatives, resulting in efficient and chemoselective N-trifluoromethylation of di- and tri-peptides with retention of configuration. A mechanism involving reductive elimination of Ag(III) intermediates to form N—CF3 bonds is proposed.

Synthesis method of amide nitrogen trifluoromethyl compound

The invention discloses a synthesis method of an amide nitrogen trifluoromethyl compound. The synthesis method comprises the following step: carrying out trifluoromethylation reaction on a compound shown in a formula a1 or a formula a2 and a trifluoromethylation reagent in an organic solvent under the action of a fluorination reagent, an oxidant, silver oxysalt and a pyridine ligand, so as to obtain a target compound shown in a formula b1 or a formula b2. According to the invention, trifluoromethylation reaction can be directly carried out on an amide compound shown as a formula a1 or a sulfonamide compound shown as a formula a2 so as to obtain the amide nitrogen trifluoromethyl compound shown in the formula b1 or the sulfamide nitrogen trifluoromethyl compound shown in the formula b2. Themethod has the advantages of simple operation, easily available raw materials, low cost, safety, environmental protection, mild reaction conditions, easy realization of large-scale production, and the like, and is of great significance to the industrial application of the amide nitrogen trifluoromethyl compound.

4- (5-CYANO-PYRAZOL-1-YL) -PIPERIDINE DERIVATIVES AS GPR 119 MODULATORS

Compounds that modulate the activity of the G-protein-coupled receptor GPR119 and their uses in the treatment of diseases linked to the modulation of the G-protein- coupled receptor GPR119 in animals are described herein.

L- ( PIPERIDIN-4-YL) -PYRAZOLE DERIVATIVES AS GPR 119 MODULATORS

Compounds of Formula I that modulate the activity of the G-protein-coupled receptor GPR119 and their uses in the treatment of diseases linked to the modulation of the G-protein-coupled receptor GPR119 in animals are described herein.

TRIAZOLE DERIVATIVE OR SALT THEREOF

[Problem] There is provided a compound which can be used for therapy of diseases in which 11 β-hydroxysteroid dehydrogenase type 1(11β-HSD1) participates, in particular diabetes, insulin resistance. [Means for Solution] It has been found that a triazole derivative wherein the triazole ring is substituted with a trisubstituted methyl group in the 2-position or a pharmaceutically acceptable salt thereof has a strong 11β-HSD1 inhibitory activity. Moreover, the triazole derivative of the invention exhibits an excellent blood-glucose level-lowering action and hence can be used for therapy of diabetes, insulin resistance.

11-BETA-HYDROXYSTEROID DEHYDROGENASE 1 INHIBITORS USEFUL FOR THE TREATMENT OF DIABETES, OBESITY AND DYSLIPIDEMIA

Compounds having Formula (I), including pharmaceutically acceptable salts, hydrates and solvates thereof, are selective inhibitors of the 11β-HSD1 enzyme. The compounds are useful for the treatment of diabetes, such as noninsulin-dependent diabetes (NIDDM), hyperglycemia, obesity, insulin resistance, dylsipidemia, hyperlipidemia, hypertension, Syndrome X, and other symptoms associated with NIDDM.