4320-90-5

Usage

Uses

Used in Pharmaceutical Research:
2H-1,2,3 Triazole-2-Acetic Acid Ethyl Ester is used as a key intermediate for the synthesis of pharmaceutical compounds, particularly due to its antifungal and antimicrobial properties. It aids in the development of new drugs targeting a range of infections and diseases.
Used in Organic Synthesis:
In the field of organic synthesis, 2H-1,2,3 Triazole-2-Acetic Acid Ethyl Ester is utilized as a building block for creating a variety of chemical compounds, contributing to the advancement of chemical research and product development.
Used in Fluorescent Dye Synthesis:
2H-1,2,3 Triazole-2-Acetic Acid Ethyl Ester is used as a component in the synthesis of fluorescent dyes, which are essential in various applications such as bioimaging, diagnostics, and other scientific research areas.
Used in Material Production:
2H-1,2,3 TRIAZOLE-2-ACETIC ACID ETHYL ESTER is also employed as a building block in the production of various materials, showcasing its versatility and importance in material science and engineering.

InChI:InChI=1/C5H8N4O2/c1-2-11-5(10)3-9-7-4-6-8-9/h4H,2-3H2,1H3

Upstream product

• 105-36-2 ethyl bromoacetate 
• 288-36-8 1 ,2,3-Triazole 
• 288-36-8 1,2,3-triazole 

Downstream Products

• 1196548-24-9 ethyl 3-(4-bromophenyl)-2-(2H-1,2,3-triazol-2-yl)propanoate 
• 610797-95-0 8-(5-Methyl-2-phenyl-oxazol-4-yl)-2-[1,2,3]triazol-2-yl-oct-4-ynoic acid ethyl ester 

Relevant academic research and scientific papers

Discovery of Molidustat (BAY 85-3934): A Small-Molecule Oral HIF-Prolyl Hydroxylase (HIF-PH) Inhibitor for the Treatment of Renal Anemia

Small-molecule inhibitors of hypoxia-inducible factor prolyl hydroxylases (HIF-PHs) are currently under clinical development as novel treatment options for chronic kidney disease (CKD) associated anemia. Inhibition of HIF-PH mimics hypoxia and leads to increased erythropoietin (EPO) expression and subsequently increased erythropoiesis. Herein we describe the discovery, synthesis, structure–activity relationship (SAR), and proposed binding mode of novel 2,4-diheteroaryl-1,2-dihydro-3H-pyrazol-3-ones as orally bioavailable HIF-PH inhibitors for the treatment of anemia. High-throughput screening of our corporate compound library identified BAY-908 as a promising hit. The lead optimization program then resulted in the identification of molidustat (BAY 85-3934), a novel small-molecule oral HIF-PH inhibitor. Molidustat is currently being investigated in clinical phase III trials as molidustat sodium for the treatment of anemia in patients with CKD.

7-OXO -6-(SULFOOXY)- 1,6-DIAZABICYCLO [3.2.1] OCTANE CONTAINING COMPOUNDS AND THEIR USE IN TREATMENT OF BACTERIAL INFECTIONS

Compounds of Formula (I) or a stereoisomer or a pharmaceutically acceptable salt thereof, their preparation, and use in treating a bacterial infection are disclosed.

Potent and selective triazole-based inhibitors of the hypoxia-inducible factor prolyl-hydroxylases with activity in the murine brain

As part of the cellular adaptation to limiting oxygen availability in animals, the expression of a large set of genes is activated by the upregulation of the hypoxia-inducible transcription factors (HIFs). Therapeutic activation of the natural human hypoxic response can be achieved by the inhibition of the hypoxia sensors for the HIF system, i.e. the HIF prolylhydroxylases (PHDs). Here, we report studies on tricyclic triazole-containing compounds as potent and selective PHD inhibitors which compete with the 2-oxoglutarate co-substrate. One compound (IOX4) induces HIFα in cells and in wildtype mice with marked induction in the brain tissue, revealing that it is useful for studies aimed at validating the upregulation of HIF for treatment of cerebral diseases including stroke.

METHOD FOR THE PREPARATION OF TRIAZOLE COMPOUNDS

The present invention relates to a process for preparing 1-[6-(morpholin-4-yl)pyrimidin-4-yl]-4-(1H-1,2,3-triazol-1-yl)-1H-pyrazol-5-ol (I—enol form) or 2-[6-(morpholin-4-yl)pyrimidin-4-yl]-4-(1H-1,2,3-triazol-1-yl)-1,2-dihydro-3H-pyrazol-3-one (I—keto form) and sodium 1-[6-(morpholin-4-yl)pyrimidin-4-yl]-4-(1H-1,2,3-triazol-1-yl)-1H-pyrazol-5-olate (II) from 1,2,3-triazole (III), methyl bromoacetate (IV-Me-Br) or ethyl bromoacetate (IV-Et-Br), 4,6-dichloropyrimidine (VIII), morpholine (IX) and hydrazine (XII).

1, 2, 4 -TRIAZOLE DERIVATIVES AS VASOPRESSIN ANTAGONISTS

Compounds of formula (I), or a pharmaceutically acceptable salt, solvate, ester or amide thereof, wherein R1 represents [CH2]n-R2; R2 represents H, C1-6 alkyloxy or Het; n represents a numb

TRIAZOLE DERIVATIVES AS VASOPRESSIN ANTAGONISTS

Compounds of formula (I), or pharmaceutically acceptable derivatives thereof, wherein: R1 represents a group selected from H, CF3, and C1-6 alkyl (optionally substituted by C1-6 alkyloxy or triazolyl); R2/

Compounds useful in therapy

Compounds of formula (I), or pharmaceutically acceptable derivatives thereof, wherein: X represents —[CH2]a—R or —[CH2]a—O—[CH2]b—R; a represents a number selected from 0 to 6; b represents a number selected from 0 to 6; R represents H, CF3 or Het; Het represents an optionally substituted 5- or 6-membered saturated, partially saturated or aromatic heterocyclic ring; Y represents one or more substituents independently selected from —[O]c—[CH2]d—R1, which may be the same or different at each occurrence; c at each occurrence independently represents a number selected from 0 or 1; d at each occurrence independently represents a number selected from 0 to 6; R1 at each occurrence independently represents H, halo, CF3, CN or Het1; Het1 at each occurrence independently represents a 5- or 6-membered unsaturated heterocyclic ring; V represents a direct link or —O—; Ring A represents an optionally substituted 5- to 7-membered saturated heterocyclic ring, or a phenylene group; Q represents a direct link or —N(R2)—; R2 represents hydrogen or C1-6 alkyl; Z represents —[O]e—[CH2]f—R3, a phenyl ring (optionally fused to a benzene ring or Het2, and the group as a whole being optionally substituted), or Het3 (optionally fused to an benzene ring or Het4, and the group as a whole being optionally substituted); R3 represents C1-6 alkyl (optionally substituted), C3-6 cycloalkyl, C3-6 cycloalkenyl, phenyl (optionally substituted), Het5 or NR4R5; e represents a number selected from 0 or 1; f represents a number selected from 0 to 6; Het2 and Het5 independently represent optionally substituted 5- or 6-membered saturated, partially saturated or aromatic heterocyclic rings; Het3 represents an optionally substituted 4 to 6-membered saturated, partially saturated or aromatic heterocyclic ring; Het4 represents an optionally substituted 6-membered aromatic heterocyclic ring; R4 and R5 independently represent optionally substituted C1-6 alkyl, C1-6 alkyloxy, C3-8 cycloalkyl (optionally fused to C3-8 cycloalkyl), Het6, or hydrogen; Het6 represents an optionally substituted 5- or 6-membered saturated, partially saturated or aromatic heterocyclic ring; are useful for treating a disorder for which a V1a antagonist is indicated.