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
• Article Data: 6

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

2-[[6-[(3R)-3-Amino-1-piperidinyl]-3,4-dihydro-3-methyl-2,4-dioxo-1(2H)-pyrimidinyl]methyl]-4-fluorobenzonitrile trifluoroacetate is a potent, selective, and noncovalent inhibitor of dipeptidyl peptidase IV (DPP-4). This inhibitor provides sustained reduction of plasma DPP-4 activity and lowering of blood glucose in animal models of diabetes.

Upstream product

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

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.

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.