924911-13-7

Usage

Type of compound

Pyrazole derivative and alcohol

Contains

Hydroxyl group

Usage

Chemical and pharmaceutical applications, building block for the synthesis of other organic compounds, reagent in laboratory research, intermediate in the production of pharmaceutical drugs

Imparts

Certain biological activity

Potential applications

Medicinal chemistry, agricultural and agrochemical industries

Upstream product

• 930-36-9 1-methyl-1H-pyrazole 
• 1072-53-3 ethyleneglycol sulfate 
• 75-21-8 oxirane 
• 924911-12-6 5-(2-{[tert-butyl(dimethyl)silyl]oxy}ethyl)-1-methyl-1H-pyrazole 

Downstream Products

• 1044856-47-4 1-methyl-4-phenyl-1,4,6,7-tetrahydropyrano[4,3-c]pyrazole 
• 1166815-99-1 6-[4-[4-[2-(1-methyl-1H-pyrazol-5-yl)ethoxy]phenyl]piperazin-1-yl]-3-(trifluoromethyl)[1,2,4]triazolo[4,3-b]pyridazine 
• 1166819-45-9 4-{4-[2-(1-methyl-1H-pyrazol-5-yl)ethoxy]phenyl}-1-[3-(trifluoromethyl)[1,2,4]triazolo[4,3-b]pyridazin-6-yl]piperidin-4-ol 
• 1166815-98-0 6-[4-[4-[2-(1-methyl-1H-pyrazol-5-yl)ethoxy]phenyl]piperidin-1-yl]-3-(trifluoromethyl)[1,2,4]triazolo[4,3-b]pyridazine 
• 16034-46-1 1-methyl-1H-pyrazole-5-carboxylic acid 
• 807315-40-8 2-(1-methyl-1H-pyrazol-5-yl)ethan-1-amine 
• 924911-14-8 5-[2-(4-allyloxy-2-methyl-benzyloxy)-ethyl]-1-methyl-1H-pyrazole 
• 924911-21-7 toluene-4-sulfonic acid 2-(2-methyl-2H-pyrazol-3-yl)-ethyl ester 

Relevant academic research and scientific papers

Synthesis and oxidation of all isomeric 2-(pyrazolyl)ethanols

[Figure not available: see fulltext.] An efficient approach to the preparation of N-substituted 2-(pyrazol-4-yl)ethanols based on recyclization reaction of 3-(dimethoxymethyl)-2-methoxytetrahydrofuran with hydrazines is described. Oxidation by KMnO4 led to 2-(pyrazol-4-yl)-2-oxoacetic acids. In contrast, 2-(pyrazol-5-yl)ethanol under similar conditions gave only pyrazole-5-carboxylic acid, which formed as a result of oxidation followed by decarbonylation. 2-(Pyrazol-3-yl)ethanol in this oxidation reaction gave a mixture of 2-oxo-2-(pyrazol-3-yl)acetic acid and pyrazole-3-carboxylic acid.

Discovery of DS-1971a, a Potent, Selective NaV1.7 Inhibitor

A highly potent, selective NaV1.7 inhibitor, DS-1971a, has been discovered. Exploration of the left-hand phenyl ring of sulfonamide derivatives (I and II) led to the discovery of novel series of cycloalkane derivatives with high NaV1.7 inhibitory potency in vitro. As the right-hand heteroaromatic ring affected the mechanism-based inhibition liability of CYP3A4, replacement of this moiety resulted in the generation of 4-pyrimidyl derivatives. Additionally, GSH adducts formation, which can cause idiosyncratic drug toxicity, was successfully avoided by this modification. An additional optimization led to the discovery of DS-1971a. In preclinical studies, DS-1971a demonstrated highly potent selective in vitro profile with robust efficacy in vivo. DS-1971a exhibited a favorable toxicological profile, which enabled multiple-dose studies of up to 600 mg bid or 400 mg tid (1200 mg/day) administered for 14 days to healthy human males. DS-1971a is expected to exert potent efficacy in patients with peripheral neuropathic pain, with a favorable safety profile.

New tetrahydropyrido pyrimidinecarboxylic compound or salt thereof

To provide a compound having an inhibitory activity for an androgen receptor. A tetrahydropyridopyrimidine compound represented by the following general formula (I) or a pharmaceutically acceptable thereof (in the formula, X and R are as defined in the specification).

TRIAZOLO [4,3-B] PYRIDAZINE DERIVATIVES AND THEIR USES FOR PROSTATE CANCER

The invention concerns bicyclic compounds of Formula (I) wherein Formula (II), R1, R2, L1, L2, J, Y, k, n, p and r are as defined in the description. The present invention also relates to processes for the preparation of such compounds, pharmaceutical compositions containing them and their use in the treatment of androgen- receptor associated conditions, particularly prostate cancer.

Novel, one-pot procedure for the synthesis of 2-arylethanol derivatives

An efficient one-pot synthesis of 2-arylethanol derivatives using ethylene sulfate as a C2 building block is described. High yields are obtained upon trapping of aryllithium intermediates generated by halogen-metal exchange or directed metalation with ethylene sulfate. The resulting heteroaryl or phenylethanol derivatives represent versatile building blocks for the synthesis of annulated pyran derivatives by oxa-Pictet-Spengler reaction.

PYRAZOLE DERIVATIVES, THEIR MANUFACTURE AND THEIR USE AS PHARMACEUTICAL AGENTS

Objects of the present invention are the compounds of formula (I), their pharmaceutically acceptable salts, enantiomeric forms, diastereoisomers and racemates, the preparation of the above-mentioned compounds, pharmaceutical compositions containing them a