1226781-80-1

Basic information

• Product Name: 2-(Methylsulfonyl)-2,4,5,6-tetrahydropyrrolo[3,4-c]pyrazole
• Synonyms: 2,4,5,6-tetrahydro-2-(methylsulfonyl)-Pyrrolo[3,4-c]pyrazole;Pyrrolo[3,4-c]pyrazole, 2,4,5,6-tetrahydro-2-(methylsulfonyl)-
• CAS NO: 1226781-80-1
• Molecular Formula: C₆H₉N₃O₂S
• Molecular Weight: 187.21956
• EINECS: -0
• Mol File: 1226781-80-1.mol

Chemical Properties

• Boiling Point: 377.5±34.0 °C(Predicted)
• Appearance: /
• Density: 1.67±0.1 g/cm3(Predicted)
• Storage Temp.: 2-8°C(protect from light)
• PKA: 6.41±0.20(Predicted)
• CAS DataBase Reference: 2-(Methylsulfonyl)-2,4,5,6-tetrahydropyrrolo[3,4-c]pyrazole(CAS DataBase Reference)
• NIST Chemistry Reference: 2-(Methylsulfonyl)-2,4,5,6-tetrahydropyrrolo[3,4-c]pyrazole(1226781-80-1)
• EPA Substance Registry System: 2-(Methylsulfonyl)-2,4,5,6-tetrahydropyrrolo[3,4-c]pyrazole(1226781-80-1)

Safety Data

• Hazardous Substances Data: 1226781-80-1(Hazardous Substances Data)

Usage

Uses

Used in Pharmaceutical Industry:
2-(Methylsulfonyl)-2,4,5,6-tetrahydropyrrolo[3,4-c]pyrazole is used as a reagent for the development of dipeptidyl peptidase IV (DPP-IV) inhibitors. These inhibitors play a crucial role in the treatment or prevention of diabetes by regulating the levels of glucose in the body. DPP-IV inhibitors help maintain a balance between the hormones responsible for glucose regulation, thus managing blood sugar levels effectively.

Upstream product

• 1226781-82-3 tert-butyl 2-(methylsulfonyl)-2,6-dihydropyrrolo[3,4-c]pyrazole-5(4H)-carboxylate 
• 1280210-79-8 2,6-dihydropyrrole [3,4-c]pyrazole-5(4H)-carboxylic acid tert-butyl ester 
• 657428-42-7 4,6-dihydro-1H-pyrrolo[3,4-c]pyrazole-5-carboxylic acid tert-butyl ester 
• 124-63-0 methanesulfonyl chloride 

Downstream Products

• 1226781-88-9 tert-Butyl {(2R,3S,5R)-2-(2,4,5-Trifluorophenyl)-5-[2-(methylsulfonyl)-2,6-dihydropyrrolo[3,4-c]pyrazol-5(4H)-yl]tetrahydro-2H-pyran-3-yl}carbamate 
• 1226781-87-8 tert-butyl {(2R,3S,5R)-2-(2,5-difluorophenyl)-5-[2-(methylsulfonyl)-2,6-dihydropyrrolo[3,4-c]pyrazol-5(4H)-yl]tetrahydro-2H-pyran-3-yl}carbamate 
• 1350652-05-9 (2R,3S,5R)-2-(2,5-difluorophenyl)-5-[2-(methylsulfonyl)-2,6-dihydropyrrolo[3,4-c]pyrazol-5(4H)-yl]thiepan-3-amine trifluoroacetate 
• 1548337-32-1 C₂₃H₂₇F₂N₅O₅S 

Relevant articles and documents

Design, Synthesis, and Evaluation of a Series of Novel Super Long-Acting DPP-4 Inhibitors for the Treatment of Type 2 Diabetes

In the present work, a novel series of trifluoromethyl-substituted tetrahydropyran derivatives were rationally designed and synthesized as potent DPP-4 inhibitors with significantly improved duration time of action over current commercially available DPP-4 inhibitors. The incorporation of the trifluoromethyl group on the 6-position of the tetrahydropyran ring of omarigliptin with the configuration of (2R,3S,5R,6S) not only significantly improves the overall pharmacokinetic profiles in mice but also maintains comparable DPP-4 inhibition activities. Further preclinical development of compound 2 exhibited its extraordinary efficacy in vivo and good safety profile. Clinical studies of compound 2 (Haisco HSK7653) are now ongoing in China, which revealed that inhibitor 2 could serve as an efficient candidate with a once-biweekly therapeutic regimen.

Aminopyran ring derivative and its composition and application wherein the dipeptidyl peptidase IV (DPP-IV) inhibitor is used for preparing the drugs for treating metabolic diseases

The present invention relates to an aminopyran ring derivative and its composition and application, specifically speaking, relating to the aminopyran ring derivative represented by the general formula (I) or its stereoisomer, pharmaceutically acceptable salt, prodrug, pharmaceutical composition containing the derivative and the preparation of dipeptidyl peptidase IV (DPP-IV) inhibitor for medical use, wherein the definitions of the substituents in the general formula (I) are the same as those defined in the patent specification.

Amino six member ring derivatives and their use in medicine (by machine translation)

The invention relates to a six-member ring amino derivatives and its application in medicine, specifically relates to the general formula (I) as shown by the six-member ring of the amino derivative or its stereoisomer, pharmaceutically acceptable salt, prodrug, pharmaceutical composition containing the derivative of the dipeptidyl peptidase IV and the preparation (dPP CGI-iV) inhibitors of their medical use, wherein the general formula (I) definition of each substituent in the definition of the description of the same. (by machine translation)

AMINO PYRANOID RING DERIVATIVE AND COMPOSITION AND USE THEREOF

The present invention relates to an amino pyran ring derivative and a composition and use thereof, and in particular, to an amino pyran ring derivative represented by general formula (I) or a stereoisomer, a pharmaceutically acceptable salt or a prodrug thereof, a pharmaceutical composition comprising the derivative, and their medical use in the manufacture of a di-peptidyl peptidase IV (DPP-IV) inhibitor, in formula (I) the substituents are defined the same as those in the specification.

Preparation method for 2-formyl chloride-2,4,5,6-tetrahydropyrrole[3,4-c]pyrazole benzene sulfonate

The invention discloses a preparation method for 2-formyl chloride-2,4,5,6-tetrahydropyrrole[3,4-c]pyrazole benzene sulfonate. The preparation method comprises the following steps: (1) adding a solvent A and dimethyl formamide-dimethyl adipate (DMF-DMA) i

AMINOTETRAHYDROPYRANS AS DIPEPTIDYL PEPTIDASE-IV INHIBITORS FOR THE TREATMENT OR PREVENTION OF DIABETES

The present invention is directed to novel substituted aminotetrahydropyrans of structural formula I which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved