736991-39-2

Usage

Uses

Used in Pharmaceutical Industry:
4-(4-Bromophenethyl)morpholine is used as a reactant for the preparation of methyllysine reader protein L3MBTL3 inhibitors. These inhibitors play a crucial role in the development of drugs targeting epigenetic regulation, which has significant implications in the treatment of various diseases, including cancer and neurological disorders.

Upstream product

• 1122-91-4 4-bromo-benzaldehyde 
• 27200-79-9 p-bromophenylacetaldehyde 
• 110-91-8 morpholine 
• 1746-28-7 1-bromo-4-(2-bromoethyl)benzene 
• 349428-85-9 2-(4-bromophenyl)-1-(morpholin-4-yl)ethan-1-one 
• 37859-24-8 2-(4-bromophenyl)acetyl chloride 
• 1878-68-8 2-(4-bromophenyl)-acetic acid 
• 5414-19-7 1,1'-oxybis(2-bromo-ethane) 
• 73918-56-6 4-Bromophenethylamine 
• 50-00-0 formaldehyd 
• 61330-38-9 morpholin-4-ium 2,2,2-trifluoroacetate 
• 115055-85-1 bromo-[(4-bromophenyl)methyl]zinc 

Downstream Products

• 364794-81-0 4-{2-[4-(4,4,5,5-tetramethyl[1,3,2] dioxaborolan-2-yl)phenyl]ethyl}morpholine 
• 1338806-02-2 (1R,2S)-(E)-5'-methoxy-2-(3-(4-(2-morpholinoethyl)styryl)-1H-indazol-6-yl)spiro(cyclopropane-1,3'-indolin)-2'-one 2,2,2-trifluoroacetate 
• 1247002-61-4 (1R,2S)-(E)-5'-methoxy-2-(3-(4-(2-morpholinoethyl)styryl)-1H-indazol-6-yl)spiro(cyclopropane-1,3'-indolin)-2'-one 
• 1247002-63-6 (E)-4-(4-(2-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)vinyl)phenethyl)morpholine 

Relevant academic research and scientific papers

B(C6F5)3-catalyzed tandem protonation/deuteration and reduction of: In situ -formed enamines

A highly efficient B(C6F5)3-catalyzed tandem protonation/deuteration and reduction of in situ-formed enamines in the presence of water and pinacolborane was developed. Regioselective β-deuteration of tertiary amines was achieved with high chemo- and regioselectivity. D2O was used as a readily available and cheap source of deuterium. Mechanistic studies indicated that B(C6F5)3 could activate water to promote the protonation and reduction of enamines. This journal is

C8-substituted pyrido[3,4-d]pyrimidin-4(3H)-ones: Studies towards the identification of potent, cell penetrant Jumonji C domain containing histone lysine demethylase 4 subfamily (KDM4)inhibitors, compound profiling in cell-based target engagement assays

Residues in the histone substrate binding sites that differ between the KDM4 and KDM5 subfamilies were identified. Subsequently, a C8-substituted pyrido[3,4-d]pyrimidin-4(3H)-one series was designed to rationally exploit these residue differences between

Derisking the Cu-Mediated 18F-Fluorination of Heterocyclic Positron Emission Tomography Radioligands

Molecules labeled with fluorine-18 (18F) are used in positron emission tomography to visualize, characterize and measure biological processes in the body. Despite recent advances in the incorporation of 18F onto arenes, the development of general and efficient approaches to label radioligands necessary for drug discovery programs remains a significant task. This full account describes a derisking approach toward the radiosynthesis of heterocyclic positron emission tomography (PET) radioligands using the copper-mediated 18F-fluorination of aryl boron reagents with 18F-fluoride as a model reaction. This approach is based on a study examining how the presence of heterocycles commonly used in drug development affects the efficiency of 18F-fluorination for a representative aryl boron reagent, and on the labeling of more than 50 (hetero)aryl boronic esters. This set of data allows for the application of this derisking strategy to the successful radiosynthesis of seven structurally complex pharmaceutically relevant heterocycle-containing molecules.

Catalytic reductive N-alkylation of amines using carboxylic acids

We report a catalytic reductive alkylation reaction of primary or secondary amines with carboxylic acids. The two-phase process involves silane mediated direct amidation followed by catalytic reduction.

SUBSTITUTED BENZAMIDES AND THEIR USES

Provided herein are Substituted Benzamides, compositions, and method of their manufacture and use.

SUBSTITUTED BENZAMIDES AND THEIR USES

Provided herein are Substituted Benzamides, compositions, and method of their manufacture and use.

The structure-activity relationships of L3MBTL3 inhibitors: Flexibility of the dimer interface

We recently reported the discovery of UNC1215, a potent and selective chemical probe for the L3MBTL3 methyllysine reader domain. In this article, we describe the development of structure-activity relationships (SAR) of a second series of potent L3MBTL3 antagonists which evolved from the structure of the chemical probe UNC1215. These compounds are selective for L3MBTL3 against a panel of methyllysine reader proteins, particularly the related MBT family proteins, L3MBTL1 and MBTD1. A co-crystal structure of L3MBTL3 and one of the most potent compounds suggests that the L3MBTL3 dimer rotates about the dimer interface to accommodate ligand binding.

New modifications to the area of pyrazole-naphthyl urea based p38 MAP kinase inhibitors that bind to the adenine/ATP site

Discovery of the pyrazole-naphthyl urea class of p38 MAP kinase inhibitors typified by the clinical candidate BIRB 796 has encouraged further exploration of this particular scaffold. Modification to the part of the inhibitor that occupies the adenine/ATP

A simple one-pot procedure for the iminium salt formation: An efficient route to β-arylethylamines

A practical and highly efficient process for the preparation of β-arylethylamines 7 was developed. Benzylic organozinc compounds 10 were reacted with the iminium salts 9 generated in situ from the amine salt 8 and paraformaldehyde in one pot and in a polar and aprotic solvent, such as NMP. A variety of the β-arylethylamines were prepared in 43-91% yields.