928201-45-0

Basic information

• Product Name: 2-[[6-[(3R)-3-AMino-1-piperidinyl]-3,4-dihydro-3-Methyl-2,4-dioxo-1(2H)-pyriMidinyl]Methyl]-4-fluorobenzonitrile Trifluoroacetate
• Synonyms: 2-[[6-[(3R)-3-AMino-1-piperidinyl]-3,4-dihydro-3-Methyl-2,4-dioxo-1(2H)-pyriMidinyl]Methyl]-4-fluorobenzonitrile Trifluoroacetate;2-[[6-[(3R)-3-AMino-1-piperidinyl]-3,4-dihydro-3-Methyl-2,4-dioxo-1(2H)-pyriMidinyl]Methyl]-4-fluorobenzonitrile Trifluoroacetic Acid Salt
• CAS NO: 928201-45-0
• Molecular Formula: C₂HF₃O₂*C₁₈H₂₀FN₅O₂
• Molecular Weight: 471.4054528
• Product Categories: Amines;Aromatics;Heterocycles;Intermediates & Fine Chemicals;Pharmaceuticals
• Mol File: 928201-45-0.mol

Chemical Properties

• Appearance: /
• CAS DataBase Reference: 2-[[6-[(3R)-3-AMino-1-piperidinyl]-3,4-dihydro-3-Methyl-2,4-dioxo-1(2H)-pyriMidinyl]Methyl]-4-fluorobenzonitrile Trifluoroacetate(CAS DataBase Reference)
• NIST Chemistry Reference: 2-[[6-[(3R)-3-AMino-1-piperidinyl]-3,4-dihydro-3-Methyl-2,4-dioxo-1(2H)-pyriMidinyl]Methyl]-4-fluorobenzonitrile Trifluoroacetate(928201-45-0)
• EPA Substance Registry System: 2-[[6-[(3R)-3-AMino-1-piperidinyl]-3,4-dihydro-3-Methyl-2,4-dioxo-1(2H)-pyriMidinyl]Methyl]-4-fluorobenzonitrile Trifluoroacetate(928201-45-0)

Safety Data

• Hazardous Substances Data: 928201-45-0(Hazardous Substances Data)

Usage

Uses

Used in Pharmaceutical Industry:
2-[[6-[(3R)-3-Amino-1-piperidinyl]-3,4-dihydro-3-methyl-2,4-dioxo-1(2H)-pyrimidinyl]methyl]-4-fluorobenzonitrile trifluoroacetate is used as a DPP-4 inhibitor for the treatment of type 2 diabetes. It provides sustained reduction of plasma DPP-4 activity and lowering of blood glucose levels in animal models of diabetes, making it a promising candidate for the development of new therapeutic agents for diabetes management.
Used in Research Applications:
In addition to its potential therapeutic applications, 2-[[6-[(3R)-3-Amino-1-piperidinyl]-3,4-dihydro-3-methyl-2,4-dioxo-1(2H)-pyrimidinyl]methyl]-4-fluorobenzonitrile trifluoroacetate is also used as a research tool in the study of DPP-4 enzyme function and its role in glucose regulation. It can help researchers gain a better understanding of the underlying mechanisms of type 2 diabetes and identify new targets for drug development.

Upstream product

• 76-05-1 trifluoroacetic acid 
• 865759-24-6 2-[(6-chloro-3-methyl-2,4-dioxo-1,2,3,4-tetrahydropyrimidin-1-yl)methyl]-4-fluorobenzonitrile 
• 334618-23-4 3-(R)-aminopiperidine dihydrochloride 
• 1261742-22-6 2-(chloromethyl)-4-fluorobenzonitrile 
• 4318-56-3 3-methyl-6-chlorouracil 

Downstream Products

• 928201-46-1 Trelagliptin hydrochloride 

Relevant articles and documents

Preparation method of dipeptidyl peptidase IV inhibitor

The invention provides a preparation method of a dipeptidyl peptidase IV inhibitor. The preparation method utilizes isopropanol and water as solvents and a volume ratio of isopropanol to water is 1-8: 1 so that a product yield and product purity are greatly improved and reaction time is shortened. An intermediate is subjected to beating and purification under action a poor solvent. The purification method is simple in operation, a product yield and product purity are high, and the production process is easy to control and is suitable for industrial production.

DIPEPTIDYL PEPTIDASE INHIBITORS

Methods of making compounds of the formula (I) wherein the variables are as defined herein. Also, methods of making compounds that may be used to inhibit dipeptidyl peptidase.

POLYMORPHS OF SUCCINATE SALT OF 2-[6-(3-AMINO-PIPERIDIN-1-YL)-3-METHYL-2,4-DIOXO-3,4-DIHYDRO-2H-PYRIMIDIN-1-YLMETHY]-4-FLUOR-BENZONITRILE AND METHODS OF USE THEREFOR

Compositions comprising the succinate salt of 2-[6-(3-Amino-piperidin-1-yl)-3-methyl-2,4-dioxo-3,4-dihydro-2H-pyrimidin-1-ylmethyl]-4-fluoro-benzonitrile (referred to herein as Compound I) which has the formula: (I) wherein the Compound I is present in one or more polymorphic forms. Also provided are novel methods for the preparation of the polymorphs of Compound I, and kits and articles of manufacture of the compositions, and methods of using the compositions to treat various diseases.

ADMINISTRATION OF DIPEPTIDYL PEPTIDASE INHIBITORS

Pharmaceutical compositions comprising 2-[6-(3-Amino-piperidin-1-yl)-3-methyl-2,4-dioxo-3,4-dihydro-2H-pyrimidin-1-ylmethyl]-4-fluoro-benzonitrile and pharmaceutically acceptable salts thereof are provided as well as kits and articles of manufacture comprising the pharmaceutical compositions as well as methods of using the pharmaceutical compositions.

ADMINISTRATION OF DIPEPTIDYL PEPTIDASE INHIBITORS

Pharmaceutical compositions comprising 2-[6-(3-Amino-piperidin-1-yl)-3-methyl-2,4-dioxo-3,4-dihydro-2H-pyrimidin-1-ylmethyl]-4-fluoro-benzonitrile and pharmaceutically acceptable salts thereof are provided as well as kits and articles of manufacture comprising the pharmaceutical compositions as well as methods of using the pharmaceutical compositions.

Dipeptidyl peptidase inhibitors

Compounds, pharmaceuticals, kits and methods are provided for use with DPP-IV and other S9 proteases that comprise a compound comprising Formula I: wherein M is N or CR4; Q1 and Q2 are each independently selected from the group consisting of CO, SO, SO2, and C=NR9; and each R1, R2, R3, R4 and R9 are as defined herein.