385425-15-0

Basic information

• Product Name: 1-(4-IODO-PHENYL)-PIPERIDIN-2-ONE
• Synonyms: 1-(4-IODO-PHENYL)-PIPERIDIN-2-ONE;1-(4-Iodophenyl)-2-piperidinone;Apixaban II;2-Piperidinone,1-(4-iodophenyl)-
• CAS NO: 385425-15-0
• Molecular Formula: C₁₁H₁₂INO
• Molecular Weight: 301.12355
• Mol File: 385425-15-0.mol

Chemical Properties

• Boiling Point: 446.1±28.0 °C(Predicted)
• Appearance: /
• Density: 1.670
• Storage Temp.: Keep in dark place,Sealed in dry,Room Temperature
• PKA: -0.43±0.20(Predicted)
• CAS DataBase Reference: 1-(4-IODO-PHENYL)-PIPERIDIN-2-ONE(CAS DataBase Reference)
• NIST Chemistry Reference: 1-(4-IODO-PHENYL)-PIPERIDIN-2-ONE(385425-15-0)
• EPA Substance Registry System: 1-(4-IODO-PHENYL)-PIPERIDIN-2-ONE(385425-15-0)

Safety Data

• HazardClass: IRRITANT
• Hazardous Substances Data: 385425-15-0(Hazardous Substances Data)

Usage

Uses

Used in Pharmaceutical Applications:
1-(4-IODO-PHENYL)-PIPERIDIN-2-ONE is used as a key intermediate in the synthesis of various bio-active molecules for pharmaceutical purposes. The enhanced biological activity due to the iodine substitution on the phenyl ring makes it a valuable compound in the development of new drugs.
Used in Research and Development:
1-(4-IODO-PHENYL)-PIPERIDIN-2-ONE is used as a research compound to study its properties, safety, and potential applications. Further research is needed to understand its full potential and to explore its use in various industries, such as pharmaceuticals, biotechnology, and materials science.
Note: Since the provided materials do not specify the exact industries or applications, the uses listed above are based on the general information provided about the compound's characteristics and potential in pharmaceutical applications. More detailed information and research would be required to identify specific industries and applications.

Upstream product

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Downstream Products

• 473927-69-4 1-(4-iodo-phenyl)-3-morpholin-4-yl-5,6-dihydro-1H-pyridin-2-one 
• 545445-44-1 5,6?dihydro?3?(4?morpholinyl)?1?[4?(2?oxo?1?piperidinyl)phenyl]?2(1H)?pyridone 
• 503614-91-3 1-(4-methoxy-phenyl)-7-oxo-6-[4-(2-oxo-piperidin-1-yl)-phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carboxylic acid ethyl ester 
• 885021-97-6 5-methoxy-2-[6-(2'-methylsulfanyl-biphenyl-4-yl)-7-oxo-3-trifluoromethyl-4,5,6,7-tetrahydro-pyrazolo[3,4-c]pyridin-1-yl]-benzenesulfonamide 
• 952040-78-7 5-methoxy-2-[6-(2'-methylsulfanyl-biphenyl-4-yl)-7-oxo-3-trifluoromethyl-4,5,6,7-tetrahydro-pyrazolo[3,4-c]pyridin-1-yl]-benzamide 

Relevant articles and documents

LACTAM-CONTAINING COMPOUNDS AND DERIVATIVES THEREOF AS FACTOR XA INHIBITORS

The present application describes lactam-containing compounds and derivatives thereof of Formula I: P4—P-M-M4??I or pharmaceutically acceptable salt forms thereof, wherein ring P, if present is a 5-7 membered carbocycle or heterocycle and ring M is a 5-7 membered carbocycle or heterocycle. Compounds of the present invention are useful as inhibitors of trypsin-like serine proteases, specifically factor Xa.

Pyrazolo [3, 4 - c] pyridine - 7 - ketone compound and use thereof

Belonging to the technical field of medicine, the invention relates to a 4, 5-dihydro-1H-pyrazolo[3, 4-c]pyridine-7-one containing derivative shown as general formula I, and pharmaceutically acceptable salt, hydrate or prodrug thereof, wherein the substituents A, R1 and R2 have meanings given in the specification. The preparation also relates to a preparation method of the general formula I compound and its pharmaceutically acceptable salt or prodrug, medicinal compositions containing the compound and application of the compound as an Xa factor inhibitor, especially application in preparation of drugs for treatment and/or prevention of thromboembolic diseases. (formula I).

Transition-Metal-Free Amine Oxidation: A Chemoselective Strategy for the Late-Stage Formation of Lactams

A metal-free strategy for the formation of lactams via selective oxidation of cyclic secondary and tertiary amines is described. Molecular iodine facilitates both chemoselective and regioselective oxidation of C-H bonds directly adjacent to a cyclic amine. The mild conditions, functional group tolerance, and substrate scope are demonstrated using a suite of diverse small molecule cyclic amines, including clinically approved drug scaffolds.

PROCESS FOR THE PREPARATION OF APIXABAN

The present invention relates to an improved process for the preparation of Apixaban and its intermediates.

AN IMPROVED PROCESS FOR THE PREPARATION OF APIXABAN

The present invention relates to an improved process for the preparation of Apixaban and its intermediates.

Novel intermediate and polymorphs of 1-(4-methoxyphenyl)-7-oxo-6-[4-(2-oxopiperidin-1-yl)phenyl]-4,5,6,7-tetra hydro-1H-pyrazolo[3,4-c]pyridine-3-carboxamide and process thereof

The present invention provides a novel intermediate as well as novel polymorphs of 1-(4-methoxyphenyl)-7-oxo-6-[4-(2-oxopiperidin-1-yl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carboxamide compound represented by the following structural formula-1 and processes for their preparation.

NOVEL PROCESS FOR THE PREPARATION OF A LACTAM-CONTAINING COMPOUND

Provided herein is a novel, commercially viable and industrially advantageous process for the preparation of 1-(4-Methoxyphenyl)-7-oxo-6-[4-(2-oxo-1-piperidinyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazole-[3,4-c]pyridine-3-carboxamide, in high yield and with high purity, using a novel intermediate 3-chloro-1-(4-iodophenyl)-5,6-dihydropyridin-2(1H)-one.

PYRAZOLE CARBOXAMIDE INHIBITORS OF FACTOR XA

The present invention relates to new pyrazole carboxamide inhibitors of factor Xa, pharmaceutical compositions thereof, and methods of use thereof.

Discovery of 1-(4-methoxyphenyl)-7-oxo-6-(4-(2-oxopiperidin-1-yl)phenyl)-4, 5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carboxamide (Apixaban, BMS-562247), a highly potent, selective, efficacious, and orally bioavailable inhibitor of blood coagulation factor Xa

Efforts to identify a suitable follow-on compound to razaxaban (compound 4) focused on modification of the carboxamido linker to eliminate potential in vivo hydrolysis to a primary aniline. Cyclization of the carboxamido linker to the novel bicyclic tetrahydropyrazolopyridinone scaffold retained the potent fXa binding activity. Exceptional potency of the series prompted an investigation of the neutral P1 moieties that resulted in the identification of the p-methoxyphenyl P1, which retained factor Xa binding affinity and good oral bioavailability. Further optimization of the C-3 pyrazole position and replacement of the terminal P4 ring with a neutral heterocycle culminated in the discovery of 1-(4-methoxyphenyl)-7-oxo-6-(4-(2-oxopiperidin-1-yl)phenyl)-4, 5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carboxamide (apixaban, compound 40). Compound 40 exhibits a high degree of fXa potency, selectivity, and efficacy and has an improved pharmacokinetic profile relative to 4.

PYRIDIL-LACTAMS AND THEIR USE 5 -HTl RECEPTORS LIGAN

The present invention relates to novel pyridyl-lactams, compounds of the formula (I), wherein R1 is a group of the formula G1, G2, G3 or G4 depicted below, and R3, Y, R6, R7, R8, R13, a, n and m are as defined herein, their pharmaceutically acceptable salts, pharmaceutical compositions, their preparation and intermediates therefrom, and their use in treating or preventing depression, anxiety, obsessive compulsive disorder (OCD) and other disorders for which a 5-HT1B antagonist is indicated.