1280210-80-1

Basic information

• Product Name: 2-(Methylsulfonyl)-2,4,5,6-tetrahydropyrrolo[3,4-c]pyrazole
• Synonyms: 2-(Methylsulfonyl)-2,4,5,6-tetrahydropyrrolo[3,4-c]pyrazole;2-(Methylsulfonyl)-2,4,5,6-tetrahydropyrrolo[3,4-c]pyrazole benzenesulfonate;MK-3102 interMediate;2-(Methylsulfonyl)-2,4,5,6-tetrahydropyrrolo[3,4-c]pyrazol-5-iuM benzenesulfonate;2,4,5,6-Tetrahydro-2-(methylsulfonyl)pyrrolo[3,4-c]pyrazole benzenesulfonate;Omarigliptin inter. OG-2;2-Methanesulfonyl-2,4,5,6-tetrahydro-pyrrolo[3,4-c]pyrazole Benzenesulfonic acid salt;Pyrrolo[3,4-c]pyrazole, 2,4,5,6-tetrahydro-2-(methylsulfonyl)-, benzenesulfonate (1:1)
• CAS NO: 1280210-80-1
• Molecular Formula: C₆H₆O₃S*C₆H₉N₃O₂S
• Molecular Weight: 345.39
• EINECS: -0
• Product Categories: intermediate
• Mol File: 1280210-80-1.mol
• Article Data: 8

Chemical Properties

• Appearance: /
• 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(1280210-80-1)
• EPA Substance Registry System: 2-(Methylsulfonyl)-2,4,5,6-tetrahydropyrrolo[3,4-c]pyrazole(1280210-80-1)

Safety Data

• Hazardous Substances Data: 1280210-80-1(Hazardous Substances Data)

Upstream product

• 905274-02-4 tert-butyl (3Z)-3-[(dimethylamino)methylene]-4-oxopyrrolidine-1-carboxylate 
• 6573-19-9 1,4,5,6-tetrahydropyrrolo[3, 4-c]pyrazole 
• 657428-42-7 4,6-dihydro-1H-pyrrolo[3,4-c]pyrazole-5-carboxylic acid tert-butyl ester 
• 124-63-0 methanesulfonyl chloride 
• 98-11-3 benzenesulfonic acid 
• 1280210-79-8 2,6-dihydropyrrole [3,4-c]pyrazole-5(4H)-carboxylic acid tert-butyl ester 
• 1226781-82-3 tert-butyl 2-(methylsulfonyl)-2,6-dihydropyrrolo[3,4-c]pyrazole-5(4H)-carboxylate 

Downstream Products

• 1226781-44-7 Omarigliptin 
• 1544022-53-8 C₂₇H₂₈F₂N₄O₄S 
• 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 
• 1280210-87-8 tert-butyl {(2R,3S)-2-(2,5-difiuorophenyl)-5-[2-(methylsulfonyl)-2,6-dihydropyrrolo[3,4-c]pyrazol-5(4H)-yl]-6-oxopiperidin-3-yl}carbamate 
• 1280210-98-1 tert-butyl [(2R,3S,5R)-2-(2,5-difiuorophenyl)-5-[2-(methylsulfonyl)-2,6-dihydropyrrolo[3,4-c]pyrazol-5(4H)-yl]-1-{2-[1-(methylsulfonyl)-1H-pyrazol-4-yl]ethyl}piperidin-3-yl]carbamate 
• 1280210-97-0 tert-butyl {(2R,3S,5R)-2-(2,5-difiuorophenyl)-5-[2-(methylsulfonyl)-2,6-dihydropyrrolo[3,4-c]pyrazol-5(4H)-yl]-1-(pyridin-2-ylmethyl)piperidin-3-yl}carbamate 
• 1280210-96-9 tert-butyl {(2R,3S,5R)-2-(2,5-difiuorophenyl)-5-[2-(methylsulfonyl)-2,6-dihydropyrrolo[3,4-c]pyrazol-5(4H)-yl]-1-(pyrazin-2-ylacetyl)piperidin-3-yl}carbamate 
• 1280210-95-8 tert-butyl {(2R,3S,5R)-1-acetyl-2-(2,5-difiuorophenyl)-5-[2-(methylsulfonyl)-2,6-dihydropyrrolo[3,4-c]pyrazol-5(4H)-yl]piperidin-3-yl}carbamate 
• 1280210-89-0 tert-butyl {(2R,3S,5S)-2-(2,5-difiuorophenyl)-5-[2-(methylsulfonyl)-2,6-dihydropyrrolo[3,4-c]pyrazol-5(4H)-yl]piperidin-3-yl}carbamate 
• 1280210-88-9 tert-butyl {(2R,3S,5R)-2-(2,5-difiuorophenyl)-5-[2-(methylsulfonyl)-2,6-dihydropyrrolo[3,4-c]pyrazol-5(4H)-yl]piperidin-3-yl}carbamate 
• 1280211-17-7 tert-butyl {(2R,3S,5R)-3-[(tert-butoxycarbonyl)amino]-2-(2,5-difiuorophenyl)-5-[2-(2-fluoro-2-methylpropyl)-2,6-dihydropyrrolo[3,4-c]pyrazol-5(4H)-yl]piperidin-1-yl}carboxylate 

Relevant articles and documents

Omarigliptin and preparation method of intermediate of Omarigliptin

The invention discloses Omarigliptin and a preparation method of an intermediate of the Omarigliptin, and provides a preparation method of an Omarigliptin intermediate I. The preparation method comprises the following step: enabling a compound II and a compound III to undergo a condensation reaction in a polar aprotic organic solvent in the presence of lewis acid and sodium borohydride acetate to obtain the Omarigliptin intermediate I. The preparation method disclosed by the invention has the advantages of simple and safe operation, no need of special purification equipment, short reaction time, fewer by products, high yield and simple post treatment operation; column chromatography separating operation in a post treatment process is avoided; a prepared product is high in purity, the optical purity is greater than or equal to 99,9 percent, the purity of a related substance is greater than or equal to 98.5 percent, and the purities of all impurities are smaller than or equal to 0.5 percent separately; the preparation method is low in production cost and is suitable for industrial production. In addition, according to the Omarigliptin prepared from the Omarigliptin intermediate I obtained by adopting the preparation method disclosed by the invention, the purity is greater than or equal to 99.5 percent, the purities of all the impurities are smaller than or equal to 0.1 percent separately, and the standards of crude drugs are reached. (The formula is shown in the description).

Crystalline forms of a dipeptidyl peptidase-IV inhibitors

Novel crystalline forms of (2R,3S,5R)-2-(2,5-Difluorophenyl)-5-[2-(methylsulfonyl)-2,6-dihydropyrrolo[3,4-c]pyrazol-5(4H)-yl]tetrahydro-2H-pyran-3-amine are potent inhibitors of dipeptidyl peptidase-IV and are useful for the treatment of non-insulin dependent (Type 2) diabetes mellitus. The invention also relates to pharmaceutical compositions containing these novel forms, processes to prepare these forms and their pharmaceutical compositions as well as uses thereof for the treatment of Type 2 diabetes.

NOVEL CRYSTALLINE FORMS OF A DIPEPTIDYL PEPTIDASE-IV INHIBITOR

Novel crystalline forms of (2R,3S,5R)-2-(2,5-Difluorophenyl)-5-[2-(methylsulfonyl)-2,6-dihydropyrrolo[3,4-c]pyrazol-5(4H)-yl]tetrahydro-2H-pyran-3-amine are potent inhibitors of dipeptidyl peptidase-IV and are useful for the treatment of non-insulin dependent (Type 2) diabetes mellitus. The invention also relates to pharmaceutical compositions containing these novel forms, processes to prepare these forms and their pharmaceutical compositions as well as uses thereof for the treatment of Type 2 diabetes.