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Trelagliptin succinate

Trelagliptin succinate Suppliers list
Company Name: Jinan Ande Pharmaceutical Co.,Ltd.
Tel: +8613256107535
Products Intro: Product Name:Trelagliptin Succinate
Purity:99% Package:1KG
Company Name: Beijing Cooperate Pharmaceutical Co.,Ltd
Tel: 010-60279497
Products Intro: Product Name:Trelagliptin Succinate
Purity:98% Package:100G;1KG;5KG;10KG;25KG;50KG;100KG
Company Name: Henan Tianfu Chemical Co.,Ltd.
Tel: 0371-55170693
Products Intro: CAS:1029877-94-8
Purity:99% Package:25KG;5KG;1KG
Company Name: Hangzhou FandaChem Co.,Ltd.
Tel: +8615858145714
Products Intro: Product Name:trelagliptin succinate
Purity:As coa Package:As request Remarks:1029877-94-8
Company Name: Nanjing ChemLin Chemical Industry Co., Ltd.
Tel: 025-83697070
Products Intro: CAS:1029877-94-8
Purity:98% Package:g-Kg Remarks:White crystal powder

Trelagliptin succinate manufacturers

  • Trelagliptin succinate
  • $30.00 / 1KG
  • 2022-04-08
  • CAS:1029877-94-8
  • Min. Order: 1KG
  • Purity: 99%
  • Supply Ability: 20 Tons
  • Trelagliptin succinate
  • $10.00 / 1kg
  • 2022-03-23
  • CAS:1029877-94-8
  • Min. Order: 1kg
  • Purity: 99%
  • Supply Ability: 10tons
Trelagliptin succinate Basic information
Product Name:Trelagliptin succinate
Synonyms:Trelagliptin Succinate (SYR-472);SYR 111472 succinate;SYR-472 succinate;Trelagliptin succinat;SYR-472 Trelagliptin succinat;Trelagliptin succinate(SRY-472);Trelagliptin succinate SYR 111472 succinate;Triglitastat succinate
Product Categories:Trelagliptin;Inhibitors;antidiabetic;API
Mol File:1029877-94-8.mol
Trelagliptin succinate Structure
Trelagliptin succinate Chemical Properties
storage temp. -20°C
color Off-white solid
Safety Information
MSDS Information
Trelagliptin succinate Usage And Synthesis
DescriptionSimilar to omarigliptin, trelagliptin succinate (XIX) is a highly selective, orally delivered inhibitor of DPP-4 developed by Takeda Pharmaceuticals and approved in Japan in March 2015 for the treatment of type 2 DM. Interestingly, trelagliptin is structurally similar to alogliptin, a DPP-4 inhibitor also marketed by Takeda and described in our 2010 review, differing only in the presence of a fluorine in the 5-position of the cyanobenzyl moiety. Both trelagliptin and alogliptin are potent inhibitors of DPP-4, with IC50s of 1.3 and 5.3 nM, respectively. Notably, while similar drugs are dosed once daily, trelagliptin is the first DPP-4 inhibitor approved for onceweekly dosing. Kinetic analysis has revealed that trelagliptin is a substrate-competitive, reversible, slow-binding inhibitor (t1/2 for dissociation = ca. 30 min) of DPP-4, although the dissociation time is insufficient to explain its long-acting effects. In a phase III trial, once-weekly trelagliptin (100 mg) showed similar efficacy and safety to once-daily alogliptin (25 mg) in patients with type 2 DM inadequately controlled by diet and exercise. The medicinal chemistry discovery of trelagliptin and alogliptin as well as reviews of this class of compounds have been published.
UsesTrelagliptin succinate (SYR-472) is a selective, long acting dipeptidyl peptidase-4 (DPP-4) inhibitor. An antidiabetic agent.
Orally active DPP-4 inhibitor that produces clinically and statistically significant improvements in glycaemic control in patients with type 2 diabetes. SYR472 has a long duration of action and is well tolerated in clinical studies.
Clinical UseTrelagliptin (SYR-472), a novel dipeptidyl peptidase-4 inhibitor used for the treatment of type 2 diabetes mellitus. Trelagliptin (as the salt Trelagliptin succinate) was approved for use in Japan in March 2015. Takeda, the company that developed Trelagliptin, chose to not get approval for the drug in the USA and EU.
Chemical SynthesisThe kilogram-scale synthesis of trelagliptin succinate has been reported in five steps from commercial starting material.102 Commercial 2-bromo-5- fluorotoluene (162) was reacted with copper cyanide in refluxing DMF to provide the corresponding nitrile in 60% yield. Benzylic bromination with AIBN and 1,3-dibromo-5,5- dimethylhydantoin (DBDMH) in DCE followed by treatment with diethyl phosphite and DIPEA gave crude benzyl bromide 163, which was substituted directly with 6-chloro-3-methyluracil (164) in the presence of DIPEA in NMP to provide chloride 165 in 86% yield. Reaction with commercial (R)-3- aminopiperidine dihydrochloride 166 in the presence of K2CO3 and i-PrOH furnished trelagliptin as the freebase. Conversion to the HCl salt and purification by crystallization from dichloromethane, followed by a freebasing via 50% NaOH, and treatment with succinic acid in THF/i-PrOH at 60 °C, and final recrystallization, generated trelagliptin succinate XIX.

ResearchTrelagliptin (Zafatek) is an orally active DPP-4 inhibitor developed by Takeda and approved in Japan for the treatment of type 2 diabetes mellitus (T2DM). Unlike other approved agents of its class, which are usually administered once daily, trelagliptin can be administered once weekly. Phase II development of trelagliptin was discontinued in the USA and EU, as Takeda considered that the costs associated with obtaining approval in these markets were prohibitive.
Trelagliptin succinate Preparation Products And Raw materials
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