827-88-3

Usage

Chemical Properties

CLEAR COLOURLESS LIQUID

InChI:InChI=1/C10H11FO/c11-9-5-3-8(4-6-9)10(12)7-1-2-7/h3-7,10,12H,1-2H2/t10-/m0/s1

Upstream product

• 772-31-6 cyclopropyl(4-fluorophenyl)methanone 
• 3874-54-2 4-(4-fluorophenyl)-4-oxo-n-butyl chloride 
• 460-00-4 1-Bromo-4-fluorobenzene 
• 1489-69-6 Cyclopropanecarboxaldehyde 
• 23719-80-4 cyclopropylmagnesium bromide 
• 459-57-4 4-fluorobenzaldehyde 
• 462-06-6 fluorobenzene 

Downstream Products

• 1108697-86-4 N-[cyclopropyl(4-fluorophenyl)methyl]-4-methylbenzenesulfonamide 
• 709-44-4 (4-Fluor-phenyl)-cyclopropyl-carbinolmethylether 
• 1202770-79-3 3-[(4-Chlorophenyl)(cyclopropyl)methyl]-5-fluoro-7-[(methylsulfonyl)methyl]-1H-indole 
• 1202770-27-1 3-[Cyclopropyl(4-fluorophenyl)methyl]-7-[(methylsulfanyl)methyl]-1H-indole 
• 298690-60-5 (+/-)-(S)-2-(4-fluorophenyl)-1-(toluene-4-sulfonyl)pyrrolidine 
• 7515-58-4 1-<4-Fluor-phenyl>--β-naphthylsulfonat 
• 7515-49-3 trans-1-(4-Fluor-phenyl)--acetat 
• 7515-50-6 (E)-4-(4-fluorophenyl)but-3-en-1-ol 
• 618068-66-9 2-(2-azido-ethyl)-3-(4-fluoro-phenyl)-oxirane 
• 536742-61-7 1-(4-fluorophenyl)pyrrolidin-3-ol 
• 70250-64-5 (E)-1-(4-chlorobut-1-en-1-yl)-4-fluorobenzene 
• 7515-48-2 (E)-1-(4-bromobut-1-en-1-yl)-4-fluorobenzene 

Relevant academic research and scientific papers

CuBr2-catalyzed ring opening/formylation reaction of cyclopropyl carbinols with DMF to synthesize formate esters

An unprecedented protocol for the synthesis of formate esters has been developed by employing N,N-dimethylformamide (DMF) as both the source of CHO and solvent. This reaction undergoes ring opening of the cyclopropyl carbinols and in situ formation of homoallylic alcohols, which reacts with DMF to give the desired products. The substrate cyclopropyl carbinols with different groups participate smoothly in this process and the desired products are obtained in moderate to good yields.

Structure-Kinetic Profiling of Haloperidol Analogues at the Human Dopamine D2 Receptor

Haloperidol is a typical antipsychotic drug (APD) associated with an increased risk of extrapyramidal side effects (EPSs) and hyperprolactinemia relative to atypical APDs such as clozapine. Both drugs are dopamine D2 receptor (D2R) antagonists, with contrasting kinetic profiles. Haloperidol displays fast association/slow dissociation at the D2R, whereas clozapine exhibits relatively slow association/fast dissociation. Recently, we have provided evidence that slow dissociation from the D2R predicts hyperprolactinemia, whereas fast association predicts EPS. Unfortunately, clozapine can cause severe side effects independent of its D2R action. Our results suggest an optimal kinetic profile for D2R antagonist APDs that avoids EPS. To begin exploring this hypothesis, we conducted a structure-kinetic relationship study of haloperidol and revealed that subtle structural modifications dramatically change binding kinetic rate constants, affording compounds with a clozapine-like kinetic profile. Thus, optimization of these kinetic parameters may allow development of novel APDs based on the haloperidol scaffold with improved side-effect profiles.

COMPOUNDS, PHARMACEUTICAL COMPOSITIONS AND USE THEREOF AS INHIBITORS OF RAN GTPASE

Compounds of general formula IA, IB and IC outlined below, including pharmaceutically acceptable salts, solvates and hydrates thereof. Such compounds and pharmaceutical compositions comprising them may be used in medical conditions involving Ran GTPase.

A method for synthesis of homoallylic bromide

Cyclopropyl Grignard reagents react with carbonyl compounds in the presence of diethyl phosphite to give homoallylic bromides. The reaction is effectively carried out under mild conditions in a one-pot fashion with moderate to good yields.

Amination of arenes through electron-deficient reaction cascades of aryl epoxyazides

(Matrix presented) Aryl epoxyazides undergo efficient electron-deficient reaction cascades mediated by Lewis acids, leading to regiospecific amination of the aromatic ring.

Quaternary ammonium antiarrhythmic drugs

Quaternary ammonium salts of certain phenylbutylamines are useful antiarrhythmic drugs. A method for treating arrhythmia and prolonging the action potential of cardiac tissue is provided. Pharmaceutical formulations containing such quaternary ammonium salts are disclosed.