951127-26-7

Usage

Uses

Used in Pharmaceutical Synthesis:
1-(2,5-difluorophenyl)-2-nitroethanol is used as a precursor for the synthesis of various pharmaceuticals, leveraging its nitro group's susceptibility to reduction reactions and the synthetic manipulations that follow, leading to a range of useful compounds.
Used in Agricultural Chemicals:
In the agricultural industry, 1-(2,5-difluorophenyl)-2-nitroethanol is used as a starting material for the development of fungicides and insecticides, taking advantage of its chemical structure to create effective pest control agents.
Used in Organofluorine Chemistry:
The presence of fluorine atoms in 1-(2,5-difluorophenyl)-2-nitroethanol allows for its application in organofluorine chemistry, where it can be used to impart desirable properties to compounds, enhancing their performance in various applications.

Upstream product

• 75-52-5 nitromethane 
• 2646-90-4 2,5-difluorobenzaldehyde 

Downstream Products

• 951127-25-6 N-[(2R,3S)-2-(2,5-difluorophenyl)tetrahydro-5-oxo-2H-pyran-3-yl]carbamic acid 1,1-dimethylethyl ester 
• 1601482-70-5 tert-butyl ((2R,3S,5R)-2-(2,5-difluorophenyl)-5-(5-(methylsulfonyl)-hexahydropyrrolo[3,4-c]pyrrol-2(1H)-yl)tetrahydro-2H-pyran-3-yl)carbamate 
• 1601479-72-4 (2R,3S,5R)-2-(2,5-difluorophenyl)-5-(5-(methylsulfonyl)hexahydropyrrolo[3,4-c]pyrrol-2(1H)-yl)tetrahydro-2H-pyran-3-amine 
• 1601482-71-6 tert-butyl ((2R,3S,5R)-2-(2,5-difluorophenyl)-5-(7-(methylsulfonyl)-2,7-diazaspiro[4.4]nonan-2-yl)tetrahydro-2H-pyran-3-yl)carbamate 
• 1601479-75-7 (2R,3S,5R)-2-(2,5-difluorophenyl)-5-(7-(methylsulfonyl)-2,7-diazaspiro[4.4]nonan-2-yl)tetrahydro-2H-pyran-3-amine 
• 1601482-72-7 tert-butyl ((2R,3S,5R)-2-(2,5-difluorophenyl)-5-(tetrahydro-1H-furo[3,4-c]pyrrol-5(3H)-yl)tetrahydro-2H-pyran-3-yl)carbamate 
• 1601479-76-8 (2R,3 S,5R)-2-(2,5-difluorophenyl)-5-(tetrahydro-1H-furo[3,4-c]pyrrol-5(3H)-yl)tetrahydro-2H-pyran-3-amine 
• 1376611-29-8 6-[(3R,4S)-3-tert-butoxycarbonylamino-4-(2,5-difluorophenyl)pyrrolidin-1-yl]-5-cyanonicotinic acid methyl ester 
• 1376611-26-5 6-[(3R,4S)-3-tert-butoxycarbonylamino-4-(2,5-difluorophenyl)pyrrolidin-1-yl]nicotinic acid methyl ester 
• 1376610-99-9 [(3R,4S)-1-[5-(cyclopropyl-{1-[5-(1,1-difluoroethyl)[1,2,4]oxadiazol-3-yl]piperidin-4-yl}carbamoyl)pyrimidin-2-yl]-4-(2,5-difluorophenyl)pyrrolidin-3-yl]carbamic acid tert-butyl ester 
• 1376610-97-7 [(3R,4S)-1-{5-[(1-cyanopiperidin-4-yl)(cyclopropyl)carbamoyl]pyrimidin-2-yl}-4-(2,5-difluorophenyl)pyrrolidin-3-yl]carbamic acid tert-butyl ester 
• 1376610-96-6 [(3R,4S)-1-{5-[(1-carbamoylpiperidin-4-yl)(cyclopropyl)carbamoyl]pyrimidin-2-yl}-4-(2,5-difluorophenyl)pyrrolidin-3-yl]carbamic acid tert-butyl ester 
• 1376608-13-7 2-[(3R,4S)-3-amino-4-(2,5-difluorophenyl)pyrrolidin-1-yl]pyrimidine-5-carboxylic acid [1-(3-isopropyl[1,2,4]oxadiazol-5-yl)piperidin-4-yl](methyl)amide 
• 1376610-75-1 {(3R,4S)-1-[5-({1-[3-(1,1-difluoroethyl)[1,2,4]oxadiazol-5-yl]piperidin-4-yl}(2,2,2-trifluoroethyl)carbamoyl)pyrimidin-2-yl]-4-(2,5-difluorophenyl)pyrrolidin-3-yl}carbamic acid tert-butyl ester 

Relevant academic research and scientific papers

Omarigliptin (MK-3102): A novel long-acting DPP-4 inhibitor for once-weekly treatment of type 2 diabetes

In our effort to discover DPP-4 inhibitors with added benefits over currently commercially available DPP-4 inhibitors, MK-3102 (omarigliptin), was identified as a potent and selective dipeptidyl peptidase 4 (DPP-4) inhibitor with an excellent pharmacokinetic profile amenable for once-weekly human dosing and selected as a clinical development candidate. This manuscript summarizes the mechanism of action, scientific rationale, medicinal chemistry, pharmacokinetic properties, and human efficacy data for omarigliptin, which is currently in phase 3 clinical development.

New method for preparing omarigliptin key intermediate

The invention provides a new method for preparing an omarigliptin key intermediate. The method comprises the following steps that 2,5-difluorobenzaldehyde is used as a raw material, and through a 7-step reaction, the omarigliptin key intermediate is obtai

AMINOTETRAHYDROPYRAN DERIVATIVE USED AS DIPEPTIDYL PEPTIDASE-IV INHIBITOR

Provided is an Aminotetrahydropyran derivative represented by general formula (I), a preparation method for the derivative, a pharmaceutical composition containing the derivative, and the use of the derivative to prepare a therapeutic agent, especially a dipeptidyl peptidase-IV inhibitor.

Amino tetrahydropyrane derivatives

The invention provides amino tetrahydropyrane derivatives, pharmaceutically-acceptable salts, hydrates, solvates, stereoisomers and prodrugs of the amino tetrahydropyrane derivatives, a preparation method of the amino tetrahydropyrane derivatives and a pharmaceutical composition containing the compounds. A formula (I) of the amino tetrahydropyrane derivatives is as shown in the specification. The compounds are capable of inhibiting activity of DPP-IV (dipeptidyl peptidase IV) and can be used for treating dipeptidyl peptidase IV associated diseases such as diabetes, obesity and other metabolic diseases.

Inhibitor for dipeptidyl peptidase-IV

The invention provides an aminotetrahydropyran derivative with a general formula (I) as described in the specification, pharmaceutically acceptable salts, hydrates, solvates and stereoisomers thereof, a preparation method for the aminotetrahydropyran derivative, and a pharmaceutical composition containing the aminotetrahydropyran derivative. The aminotetrahydropyran derivative provided by the invention can inhibit the activity of dipeptidyl peptidase-IV(DPP-IV), and can be used for treatment of diseases related to dipeptidyl peptidase-IV, especially for treatment of diabetes.

Aminotetrahydropyrane derivatives and medical applications thereof

The invention discloses aminotetrahydropyrane derivatives and medical applications thereof. The invention relates to substituted aminotetrahydropyrane with a novel structural formula (I). The substituted aminotetrahydropyrane can be used as an inhibitor of dipeptidyl peptidase-IV, and can be applied to treatment or prevention of diseases related with dipeptidyl peptidase-IV, such as diabetes, especially type II diabetes. The invention also relates to a pharmaceutical composition comprising the aminotetrahydropyrane derivatives, and an application of the compounds and the composition in the treatment or prevention of diseases related with dipeptidyl peptidase-IV.

Vasicine from Adhatoda vasica as an organocatalyst for metal-free Henry reaction and reductive heterocyclization of o-nitroacylbenzenes

Vasicine, a quinazoline alkaloid, from the leaves of Adhatoda vasica, has been utilized as an efficient catalyst for metal and base free Henry reaction of various aldehydes with nitro alkanes. The method can be used in the synthesis of various β-nitro alcohols under mild reaction conditions without use of hazardous organic solvents and expensive catalysts. Vasicine is also applied successfully for one pot synthesis of 2,1-benzisoxazoles from o-nitroacylbenzenes in good yields under mild conditions.

Aminotetrahydropyran derivative used as dipeptidyl peptidase-IV inhibitor

The invention provides an aminotetrahydropyran derivative as shown in the general formula (I), pharmaceutically acceptable salt, hydrate, solvate and stereisomer of the derivative, a preparation method thereof, and a pharmaceutical composition containing the compound. The compound can inhibit activity of dipeptidyl peptidase IV (DPP-IV) and can be used in treating diseases related to dipeptidyl peptidase IV.

2-PHENYL-5-HETEROCYCLYL-TETRAHYDRO-2H-PYRAN-3-AMINE COMPOUNDS FOR USE IN THE TREATMENT OF DIABETES AND ITS ASSOCIATED DISORDERS

The present invention relates to novel compounds of the general formula (I) their tautomeric forms, their enantiomers, their diastereoisomers, their pharmaceutically accepted salts, or pro-drugs thereof, which are useful for the treatment or prevention of diabetes mellitus (DM), obesity and other metabolic disorders. The invention also relates to process for the manufacture of said compounds, and pharmaceutical compositions containing them and their use.

1,4 DISUBSTITUTED PYRROLIDINE - 3 - YL -AMINE DERIVATIVES AND THEIR USE FOR THE TREATMENT OF METABOLIC DISORDERS

Therapeutic compounds are disclosed having the general formula (I) that are useful for the treatment of metabolic disorders, including type II diabetes. The compounds have activity as agonists of GPR1 19. Compounds having stereochemistry of formula (la) may also demonstrate DPP-IV inhibitory activity.