666816-91-7

Usage

Uses

Used in Pharmaceutical Industry:
Linagliptin Impurity D is used as a synthetic compound for the development and production of Linagliptin, an antidiabetic drug. It plays a crucial role in the synthesis process, contributing to the overall efficacy and safety of the final product.
Additionally, Linagliptin Impurity D may be utilized in research and development for the discovery of new pharmaceutical compounds with potential therapeutic applications. Its unique chemical structure and properties make it a valuable tool for exploring novel drug candidates and advancing the field of medicinal chemistry.

Upstream product

• 309956-78-3 (R)-piperidin-3-ylcarbamic acid tert-butyl ester 
• 666816-98-4 8-bromo-7-(but2-yn-1-yl)-3-methyl-3,7-dihydro-1H-purine-2,6–dione 
• 93703-24-3 3-methyl-8-bromoxanthine 

Downstream Products

• 668270-12-0 Linagliptin 

Relevant academic research and scientific papers

A preparation method of advantage geleg sandbank

The invention discloses a preparation method for Trajenta. The Trajenta is a high-purity Trajenta which is prepared by taking a raw material 8-bromo-7-(2-butynyl)-3-methylxanthine, namely a compound a as basic material, selecting appreciate reaction material ratio, reaction time and reaction conditions in substitution, deprotection and other reaction steps. The preparation method has the beneficial effects that a novel method for preparing the Trajenta is provided, and dimer impurities generated in the reaction process are effectively avoided, so that the high-purity Trajenta is obtained, the raw material of the reaction are easily available, the production cost is low, and industrial production requirement of the Trajenta can be met to the greatest extent.

Xanthine derivatives, their preparation and use

The present invention relates to a xanthine derivative, a pharmaceutically acceptable salt thereof, a solvate of the derivative, a solvate of the pharmaceutically acceptable salt, a chemically protected form or prodrug thereof and a preparation method and a use thereof; and also relates to an intermediate compound used for preparing the xanthine derivative and a preparation method of the intermediate compound. The xanthine derivative and a pharmaceutical composition thereof effectively inhibit the activity of DPP-IV, and can be used for preparing a drug for diseases associated with dipeptidyl peptidase (DPP-IV).

METHOD FOR PREPARING AN IMPORTANT INTERMEDIATE OF LINAGLIPTIN

The present invention discloses an improved process for preparing an important intermediate of linagliptin. In particular, disclosed are a process for preparing a compound V which is an important intermediate of linagliptin and has the structure V, and an industrial process of preparing linagliptin having excellent chemical and optical purities, which is an inhibitor of dipeptidyl peptidase-4 (DPP-IV), from the compound V. The process employs a phase-transfer catalyst, is high in yield, easy and simple to handle, environmentally friendly, suitable for industrial mass production, and can be implemented by a “one-pot process”.

8-[3-AMINO-PIPERIDIN-1-YL]-XANTHINE, THE PRODUCTION THEREOF AND THE USE IN THE FORM OF A DPP INHIBITOR

The invention relates to substituted xanthines of general formula (I), wherein R is such as defined in claim 1, and to the tautomers, stereoisomers, mixtures and the salts thereof, said products exhibiting precious pharmacological properties, in particular an inhibiting effect on a dipeptidylpeptidasa-IV (DPP-IV) enzyme activity.

8-[3-amino-piperidin-1-yl]-xanthines, their preparation and their use as pharmaceutical compositions

The present invention relates to substituted xanthines of general formula wherein R is defined as in claim 1, the tautomers, the stereoisomers, the mixtures thereof and the salts thereof, which have valuable pharmacological properties, particularly an inhibiting effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).

Bicyclic imidazole derivatives, the preparation thereof and their use as pharmaceutical compositions

The present invention relates to bicyclic imidazole compounds of general formula wherein R1 to R3 and A are defined as in claims 1 to 8, the tautomers, the enantiomers, the stereoisomers, the mixtures thereof and the salts thereof, which have valuable pharmacological properties, particularly an inhibiting effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).

XANTHINE DERIVATIVES, PRODUCTION THEREOF AND USE THEREOF AS MEDICINES

The invention concerns substituted xanthines of general formula (I), wherein: R1 to R4 are such as defined in Claim 1, and tautomers, stereoisomers, mixtures, prodrugs and salts thereof. Said compounds have advantageous pharmacological properties, in particular an inhibiting effect on the activity of the dipeptidyl peptidase IV (DPP-IV) enzyme.

NOVEL XANTHINE DERIVATIVES, THE PRODUCTION AND THE USE THEREOF IN THE FORM OF DRUGS

The invention relates to xanthines presented by a general formula (I), wherein R1 to R4 are equal to these defined in the claim n° 1, and to tautomers, stereoisomers, mixtures, pro-drugs and the salts thereof. Said compounds exhibit advantages pharmacological properties, in particular an inhibiting action on the activity of enzyme dipeptidylpeptidasa-IV (DPP-IV).

NOVEL XANTHIN DERIVATIVES, PRODUCTION AND USE THEREOF AS MEDICAMENTS

The invention relates to substituted xanthins of general formula (I) wherein R1 - R4 are defined as in Claim 1, the tautomers thereof, the stereoisomers thereof, the mixtures thereof, the prodrugs and salts thereof which exhibit valuable pharmacological properties, especially an inhibitive effect on the activity of the enzyme Dipeptidylpeptidase-IV (DPP-IV).