928201-46-1

Basic information

• Product Name: Trelagliptin hydrochloride
• Synonyms: Trelagliptin hydrochloride
• CAS NO: 928201-46-1
• Molecular Weight: 393.848
• Mol File: 928201-46-1.mol

Chemical Properties

• CAS DataBase Reference: Trelagliptin hydrochloride(CAS DataBase Reference)
• NIST Chemistry Reference: Trelagliptin hydrochloride(928201-46-1)
• EPA Substance Registry System: Trelagliptin hydrochloride(928201-46-1)

Safety Data

• Hazardous Substances Data: 928201-46-1(Hazardous Substances Data)

Upstream product

• 865759-24-6 2-[(6-chloro-3-methyl-2,4-dioxo-1,2,3,4-tetrahydropyrimidin-1-yl)methyl]-4-fluorobenzonitrile 
• 421552-12-7 2-(bromomethyl)-4-fluorobenzonitrile 
• 452-63-1 2-Bromo-5-fluorotoluene 
• 147754-12-9 4-fluoro-2-methylbenzonitrile 
• 928201-45-0 Trelagliptin trifluoroacetate 

Relevant articles and documents

New trelagliptin preparation process

The present invention provides a trelagliptin preparation process, which comprises that: 1) a compound 4 and a compound 5 are adopted as raw materials, and are subjected to a condensation reaction in an organic solvent in the presence of an alkali to obtain a compound 6; 2) the compound 6 reacts with an acid HA in an organic solvent to remove the t-butyloxy carbonyl so as to obtain a trelagliptin.HA salt; and 3) the trelagliptin.HA salt is subjected to alkali neutralization treatment and purification to obtain the trelagliptin, wherein the reaction route is defined in the specification. According to the present invention, in the improved preparation process, the 2-site amino of the compound 5 is protected by the t-butyloxy carbonyl, such that the selectivity of the nucleophilic substitution reaction is improved, and the impurity production caused by primary amine substitution is avoided so as to improve the nucleophilic substitution yield and improve the trelagliptin purity.

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.

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.