328546-72-1

Upstream product

• 364-78-3 2-nitro-4-fluoroaniline 
• 100-85-6 N-benzyl-trimethylammonium hydroxide 
• 107-13-1 acrylonitrile 

Downstream Products

• 205701-85-5 RWJ 51204 
• 155202-16-7 7-fluoro-N-(2-fluorophenyl)-1,2,3,5-tetrahydro-3-oxopyrido[1,2-a]benzimidazole-4-carboxamide 
• 328546-73-2 N-(4-fluoro-2-nitrophenyl)-β-alanine 

Relevant academic research and scientific papers

Tricyclic benzimidazoles and their use as metabotropic glutamate receptor modulators

The invention provides for a compound of formula (I) or a pharmaceutically acceptable salt thereof: wherein R1, R2, R3, A, B, D, m, n, x, and y are defined as described in the specification. The invention additionally provides a pharmaceutically composition comprising the compound of formula I, together with a method of using the same to treat or prevent neurological and psychiatric disorders. The compounds are useful in therapy related to the treatment or prevention of mGluR2 receptor-mediated disorders.

4,5-DIHYDRO-IMIDAZO[4,5,1-II]QUINOLIN-6-ONES AS PARP INHIBITORS

Compounds of the formula 1, in which R1 and R2 have the meanings indicated in the description, are novel active PARP inhibitors.

Tricyclic inhibitors of poly(ADP-ribose) polymerases

Compounds of the formula shown below are poly(ADP-ribosyl)transferase inhibitors: Such compounds are useful as therapeutics in treating cancers and in ameliorating the effects of stroke, head trauma, and neurodegenerative disease.

Process research for the synthesis of RWJ-51204, a novel anxiolytic agent

RWJ-51204, the lead compound in our pyrido [1,2-α] benzimidazole (PBI) series, was shown to exhibit anxiolytic efficacy in animal models at doses which did not cause central nervous system side effects commonly observed with other anxiolytic agents. To prepare supplies of drug substance for early toxicological and clinical studies, we needed to develop a safe and scaleable synthesis. Our main focus was to improve the last two steps of the process which involved formation of the penultimate carboxamide intermediate followed by alkylation using potentially toxic chloromethyl ethyl ether. Due to safety issues concerning storage and handling of this reagent during the large scale synthesis, we investigated alternate routes to minimize potential exposure risks. The process research carried out for the final steps that led to the safe and cost-effective multi-kilogram synthesis of RWJ-51204 is described herein.