235109-63-4

Usage

Piperidine derivative

A chemical compound derived from piperidine, which is a heterocyclic organic compound that consists of a six-membered ring containing five carbon atoms and one nitrogen atom.

BOC protecting group

The compound contains a tert-butyloxycarbonyl (BOC) group, which is a protecting group used in organic synthesis to temporarily block the reactivity of an amine or alcohol functional group.

Intermediate in synthesis

1-N-BOC-4-(4-CHLOROPHENYL)-4-HYDROXYPIPERIDINE is primarily used as an intermediate in the synthesis of pharmaceutical drugs and other organic compounds, meaning it is a precursor that reacts further to form the final product.

Potential applications in medicinal chemistry

Due to its structural features, 1-N-BOC-4-(4-chlorophenyl)-4-hydroxypiperidine has potential applications in the development of new drugs and the study of medicinal chemistry.

Biological activity and pharmacological properties

The 4-(4-chlorophenyl)-4-hydroxypiperidine moiety in the compound may impart biological activity and pharmacological properties, making it a valuable building block for the synthesis of new drug candidates.

Versatile and important chemical compound

1-N-BOC-4-(4-chlorophenyl)-4-hydroxypiperidine is a significant compound in the fields of organic and medicinal chemistry due to its unique structure and potential applications.

Upstream product

• 106-39-8 bromochlorobenzene 
• 79099-07-3 N-tert-butyloxycarbonylpiperidin-4-one 
• 39512-49-7 4-(4-chlorophenyl)-4-hydroxypiperidine 
• 24424-99-5 di-tert-butyl dicarbonate 
• 637-87-6 1-Chloro-4-iodobenzene 
• 873-77-8 (4-chlorphenyl)magnesium bromide 

Downstream Products

• 235109-80-5 4-(4-chloro-phenyl)-4-methoxy-piperidine 
• 946593-11-9 tert-butyl 4-(4-chlorophenyl)piperidine-1-carboxylate 
• 26905-02-2 4-(4-chlorophenyl)piperidine 
• 771-99-3 4-phenylpiperidine 
• 34104-67-1 reduced haloperidol 
• 59995-68-5 Chlorohaloperidol 
• 5957-96-0 4-(4-chlorophenyl)pyridine 
• 917925-59-8 tert-butyl 4-amino-4-(4-chlorophenyl)piperidine-1-carboxylate 
• 1076199-00-2 benzyl 4-(4-chlorophenyl)-4-hydroxypiperidine-1-carboxylate 
• 1345609-64-4 2-benzyl-3-[4-(4-chlorophenyl)-4-fluoropiperidin-1-yl]propionic acid hydrochloride 
• 1345610-15-2 methyl 2-benzyl-3-[4-(4-chlorophenyl)-4-fluoropiperidin-1-yl]propionate hydrochloride 
• 1345610-13-0 methyl 3-[4-(4-chlorophenyl)-4-fluoropiperidin-1-yl]propionate 
• 1345610-11-8 4-(4-chlorophenyl)-1-(3,3-diphenylpropyl)-4-fluoropiperidine 
• 1345609-57-5 4-(4-chlorophenyl)-1-(3,3-diphenylpropyl)-4-fluoropiperidine hydrochloride 

Relevant academic research and scientific papers

Light-Mediated Formal Radical Deoxyfluorination of Tertiary Alcohols through Selective Single-Electron Oxidation with TEDA2+.

The synthesis of tertiary alkyl fluorides through a formal radical deoxyfluorination process is described herein. This light-mediated, catalyst-free methodology is fast and broadly applicable allowing for the preparation of C?F bonds from (hetero)benzylic, propargylic, and non-activated tertiary alcohol derivatives. Preliminary mechanistic studies support that the key step of the reaction is the single-electron oxidation of cesium oxalates—which are readily available from the corresponding tertiary alcohols—with in situ generated TEDA2+. (TEDA: N-(chloromethyl)triethylenediamine), a radical cation derived from Selectfluor.

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.

Monoamine Oxidase (MAO-N) Whole Cell Biocatalyzed Aromatization of 1,2,5,6-Tetrahydropyridines into Pyridines

A sustainable MAO-N biocatalyzed process for the synthesis of pyridines from aliphatic tetrahydropyridines (THP) has been developed. Pyridine compounds were synthesized under mild reaction conditions and with high conversion, exploiting MAO-N whole cells as aromatizing biocatalysts. The kinetic profile of the whole cell biocatalytic transformation was finally investigated via in situ 19F NMR.

A Versatile Route to Unstable Diazo Compounds via Oxadiazolines and their Use in Aryl–Alkyl Cross-Coupling Reactions

Coupling of readily available boronic acids and diazo compounds has emerged recently as a powerful metal-free carbon–carbon bond forming method. However, the difficulty in forming the unstable diazo compound partner in a mild fashion has hitherto limited their general use and the scope of the transformation. Here, we report the application of oxadiazolines as precursors for the generation of an unstable family of diazo compounds using flow UV photolysis and their first use in divergent protodeboronative and oxidative C(sp2)?C(sp3) cross-coupling processes, with excellent functional-group tolerance.

METALLO-BETA-LACTAMASE INHIBITORS

The present invention relates to compounds of formula (I) that are metallo-β-lactamase inhibitors, the synthesis of such compounds, and the use of such compounds for use with β-lactam antibiotics for overcoming resistance.

METALLO-BETA-LACTAMASE INHIBITORS

The present invention relates to compounds of formula (I) that are metallo-β-lactamase inhibitors, the synthesis of such compounds, and the use of such compounds for use with β-lactam antibiotics for overcoming resistance.

HETEROCYCLIC MODULATORS OF LIPID SYNTHESIS AND COMBINATIONS THEREOF

Heterocyclic modulators of lipid synthesis are provided as well as pharmaceutically acceptable salts thereof; pharmaceutical compositions comprising such compounds; and methods of treating conditions characterized by disregulation of a fatty acid synthase pathway by the administration of such compounds and combinations of such compounds and other therapeutic agents.

HETEROCYCLIC MODULATORS OF LIPID SYNTHESIS

Heterocyclic modulators of lipid synthesis are provided as well as pharmaceutically acceptable salts thereof; pharmaceutical compositions comprising such compounds; and methods of treating conditions characterized by disregulation of a fatty acid synthase pathway by the administration of such compounds.

COMBINATIONS OF MEDICAMENTS, CONTAINING PDE4-INHIBITORS AND EP4-RECEPTOR-ANTAGONISTS

The present invention relates to new medicament combinations which contain in addition to one or more PDE4-inhibitors (1) at least one EP4 receptor antagonist (2), as well as the use thereof for the treatment of preferably respiratory complaints such as particularly COPD, chronic sinusitis and asthma. The invention relates in particular to those medicament combinations which contain, in addition to one or more, preferably one, PDE4 inhibitor of general formula 1 wherein X is SO or SO2, but preferably SO, and wherein R1, R2, R3 and R4 have the meanings given in claim 1, at least one EP4 receptor antagonist (2), the preparation thereof and the use thereof for the treatment of respiratory complaints.

DRUG COMBINATIONS CONTAINING PDE4 INHIBITORS AND NSAIDS

The present invention relates to new drug combinations which contain in addition to one or more PDE4-inhibitors at least one NSAID (=non-steroidal anti-inflammatory drug) (2), processes for preparing them and their use in treating in particular respiratory complaints such as for example COPD, chronic sinusitis and asthma. The invention particularly relates to those drug combinations which contain, in addition to one or more, preferably one PDE4 inhibitor of general formula 1 wherein X is SO or SO2, but preferably SO, and wherein R1, R2, R3 and R4 have the meanings given in claim 1, at least one NSAID (2), the preparation thereof and the use thereof for the treatment of respiratory complaints.