1215098-77-3

Usage

Molecular class

Phenylalkanoic acid

Structure

Five-carbon chain with a chloro group at the 5th position and a 4-bromo-phenyl group at the 2nd position

Usage

Building block in organic synthesis for pharmaceuticals and agrochemicals

Biological activities

Inhibition of enzymes, potential as an antiproliferative agent

Precautions

May pose risks to human health and the environment if not properly managed

Upstream product

• 109-70-6 1.3-chlorobromopropane 
• 1878-68-8 2-(4-bromophenyl)-acetic acid 
• 14062-25-0 Ethyl 4-bromophenylacetate 
• 1215098-76-2 2-(4-bromo-phenyl)-5-chloro-pentane nitrile 

Downstream Products

• 1262106-80-8 8-(4-bromophenyl)-3-[3-methoxy-4-(2-methyl-1,3-oxazol-5-yl)phenyl]-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridine 
• 1262106-64-8 3-[3-methoxy-4-(2-methyl-1;3-oxazol-5-yl)phenyl]-8-(4-morpholin-4-ylphenyl)-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridine 
• 1215098-78-4 2-(4-bromo-phenyl)-5-chloro-pentanoic acid methyl ester 

Relevant academic research and scientific papers

Discovery of novel 5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridine derivatives as γ-secretase modulators

Novel 5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridine derivatives were designed, synthesized, and evaluated as γ-secretase modulators (GSMs). An optimization study of this series resulted in the identification of (R)-11j, which showed a potent Aβ42-lowering effect, high bioavailability and good blood-brain barrier permeability in mice. Oral administration of (R)-11j significantly reduced brain Aβ42 in mice at a dose of 10 mg/kg.

Process development of C-N cross-coupling and enantioselective biocatalytic reactions for the asymmetric synthesis of niraparib

Process development of the synthesis of the orally active poly(ADP-ribose)polymerase inhibitor niraparib is described. Two new asymmetric routes are reported, which converge on a high-yielding, regioselective, copper-catalyzed Narylation of an indazole derivative as the late-stage fragment coupling step. Novel transaminase-mediated dynamic kinetic resolutions of racemic aldehyde surrogates provided enantioselective syntheses of the 3-aryl-piperidine coupling partner. Conversion of the C-N cross-coupling product to the final API was achieved by deprotection and salt metathesis to isolate the desired crystalline salt form.

NOVEL ORTHO-AMINOANILIDES FOR THE TREATMENT OF CANCER

The present invention is directed to a compound of formula I, and processes for the manufacture of said compounds as well as medicaments containing said compound. The compounds according to this invention show anti-proliferative and differentiation-induci