313657-51-1

Usage

Uses

Used in Pharmaceutical Synthesis:
1-(2-Hydroxy-Phenyl)-Piperazin-4-Carboxylic Acid tert-Butyl Ester is used as an intermediate in the synthesis of 2-(1-Piperazinyl)-Benzenethiol (P480550), which is further used to prepare 3,5-Dioxo-(2H,4H)-1,2,4-Triazine derivatives. These derivatives act as 5-HT1AR ligands, playing a crucial role in the development of drugs targeting the serotonin receptor, which has implications in treating various neurological and psychiatric disorders.
Used in Osteoporosis Treatment:
1-(2-Hydroxy-Phenyl)-Piperazin-4-Carboxylic Acid tert-Butyl Ester is also utilized in the preparation of nonpeptidic biaryl inhibitors of human cathepsin K. These inhibitors are relevant to the treatment of osteoporosis, as they can help regulate bone resorption and maintain bone health by targeting the enzyme responsible for breaking down bone tissue.

Upstream product

• 1011-17-2 2-hydroxyphenylpiperazine 
• 24424-99-5 di-tert-butyl dicarbonate 
• 58260-69-8 1-(2-hydroxyphenyl)piperazine dihydrobromide 
• 95-56-7 2-hydroxybromobenzene 
• 57260-71-6 1-t-Butoxycarbonylpiperazine 
• 444582-88-1 1-tert-butoxycarbonyl-4-(2-(benzyloxy)phenyl)piperazine 

Downstream Products

• 444582-86-9 1-tert-butoxycarbonyl-4-[2-((1-methyl-1H-imidazol-2-yl)methoxy)phenyl]piperazine 
• 444582-88-1 1-tert-butoxycarbonyl-4-(2-(benzyloxy)phenyl)piperazine 
• 1106056-84-1 4-[2-(1-ethyl-pyrrolidin-3-yloxy)-phenyl]-piperazine-1-carboxylic acid tert-butyl ester 
• 444606-02-4 4-[2-(2-morpholin-4yl-ethoxy)-phenyl]-piperazine-1-carboxylic acid tert-butyl ester 
• 1106056-86-3 4-[2-(1-methyl-pyrrolidin-3-yloxy)-phenyl]-piperazine-1-carboxylic acid tert-butyl ester 
• 444606-74-0 N-{2-[2-(dimethylamino)ethoxy]phenyl}piperazine 
• 811828-29-2 3-[2-(4-t-butoxycarbonyl-piperazin-1-yl)-phenoxy]-1-(4-trifluoromethyl-phenyl)-pyrrolidin-2-one 
• 1106056-81-8 4-[2-(1-methyl-piperidin-4-yloxy)-phenyl]-piperazine-1-carboxylic acid tert-butyl ester 
• 1106056-83-0 4-[2-(1-methyl-piperidin-2-ylmethoxy)-phenyl]-piperazine-1-carboxylic acid tert-butyl ester 
• 1106056-85-2 4-[2-(2-pyrrolidin-1-yl-ethoxy)-phenyl]-piperazine-1-carboxylic acid tert-butyl ester 
• 597584-72-0 tert-butyl 4-(2-{[(trifluoromethyl)sulfonyl]oxy}phenyl)piperazine-1-carboxylate 
• 313657-49-7 1-[2-(2-Phenoxyethoxy)phenyl]piperazine, Hydrochloride 
• 1008509-21-4 tert-butyl 4-[2-ethoxycarbonylmethoxy-phenyl]piperazine-1-carboxylate 
• 1085928-12-6 tert-butyl 4-(2-(4-ethoxy-4-oxobutoxy)phenyl)piperazine-1-carboxylate 

Relevant academic research and scientific papers

Affinity-Based Selectivity Profiling of an In-Class Selective Competitive Inhibitor of Acyl Protein Thioesterase 2

Activity-based protein profiling (ABPP) has revolutionized the discovery and optimization of active-site ligands across distinct enzyme families, providing a robust platform for in-class selectivity profiling. Nonetheless, this approach is less straightfo

Identification of novel GLUT inhibitors

The compound class of 1H-pyrazolo[3,4-d]pyrimidines was identified using HTS as very potent inhibitors of facilitated glucose transporter 1 (GLUT1). Extensive structure–activity relationship studies (SAR) of each ring system of the molecular framework was established revealing essential structural motives (i.e., ortho-methoxy substituted benzene, piperazine and pyrimidine). The selectivity against GLUT2 was excellent and initial in vitro and in vivo pharmacokinetic (PK) studies are encouraging.

5HT1A ANTAGONIST USEFUL FOR IN VIVO IMAGING

The present invention provides a novel compound of formula (I) useful for in vivo imaging of 5-HT1 A receptors in a subject. Also provided by the present invention is a precursor compound useful in the preparation of the compound of the inventi

NOVEL SYNTHESIS METHOD

The present invention relates to a method of making compounds having affinity for the 1 A subtype of the serotonin receptor, i.e. 5HT1A. The method of the present invention provides advantages over the known methods of synthesis. The compounds

Discovery of 3-aryl-5-acylpiperazinyl-pyrazoles as antagonists to the NK3 receptor

A series of 3-aryl-5-acylpiperazinyl-pyrazoles (e.g., 3a-b) initially identified through a high-throughput screening campaign using the aequorin Ca2+ bioluminescence assay as novel, potent small molecule antagonists of the G protein-coupled hum

Compositions, Synthesis, And Methods Of Using Piperazine Based Antipsychotic Agents

The present invention provides novel piperazine derivatives which can be advantageously used for treating schizophrenia and related psychoses such as acute manic, bipolar disorder, autistic disorder and depression.

Synthesis of novel WAY 100635 derivatives containing a norbornene group and radiofluorination of [18F]AH1.MZ as a serotonin 5-HT1A receptor antagonist for molecular imaging

5-HT1A receptors are involved in a variety of psychiatric disorders and in vivo molecular imaging of the 5-HT1A status represents an important approach to analyze and treat these disorders. We report herein the synthesis of three new

COMPSITIONS, SYNTHESIS, AND METHODS OF USING QUINOLINE BASED ATYPICAL ANTIPSYCHOTIC AGENTS

The present invention provides novel quinolinone derivatives which can be advantageously used for treating schizophrenia and related psychoses such as acute manic, bipolar disorder, autistic disorder, and depression.

1,2-Di(cyclic)substituted benzene compounds

In one aspect, the present invention provides compounds having formula (1) or (100), a salt thereof or a hydrate of the foregoing, which compounds exhibit excellent cell adhesion inhibitory action or cell infiltration inhibitory action, and are useful as therapeutic or prophylactic agents for various inflammatory diseases and autoimmune diseases associated with adhesion and infiltration of leukocytes, such as inflammatory bowel disease (particularly ulcerative colitis or Crohn's disease), irritable bowel syndrome; rheumatoid arthritis, psoriasis, multiple sclerosis, asthma and atopic dermatitis. wherein R10 represents optionally substituted cycloalkyl, etc., R20-23 represent hydrogen, alkyl, alkoxy, etc., R30-32 represent hydrogen, alkyl, oxo, etc., and R40 represents optionally substituted alkyl, etc.

Synthesis and Structure-Activity Relationships of Novel Arylpiperazines as Potent and Selective Agonists of the Melanocortin Subtype-4 Receptor

The melanocortin receptors have been implicated as potential targets for a number of important therapeutic indications, including inflammation, sexual dysfunction, and obesity. We identified compound 1, an arylpiperazine attached to the dipeptide H-D-Tic-D-p-Cl-Phe-OH, as a novel melanocortin subtype-4 receptor (MC4R) agonist through iterative directed screening of nonpeptidyl G-protein-coupled receptor biased libraries. Structure-activity relationship (SAR) studies demonstrated that substitutions at the ortho position of the aryl ring improved binding and functional potency. For example, the o-isopropyl-substituted compound 29 (Ki = 720 nM) possessed 9-fold better binding affinity compared to the unsubstituted aryl ring (Ki = 6600 nM). Sulfonamide 39 (Ki = 220 nM) fills this space with a polar substituent, resulting in a further 2-fold improvement in binding affinity. The most potent compounds such as the diethylamine 44 (Ki = 60 nM) contain a basic group at this position. Basic heterocycles such as the imidazole 50 (Ki = 110 nM) were similarly effective. We also demonstrated good oral bioavailability for sulfonamide 39.