100191-61-5

Upstream product

• 6280-89-3 2-chloro-5-methoxybenzoic acid 

Downstream Products

• 103029-98-7 1-(2-chloro-5-methoxy-phenyl)-2-diazo-ethanone 
• 77344-69-5 5-methoxy-o-chloroacetophenone 
• 91367-10-1 2-(2-chloro-5-methoxy-phenyl)acetic acid 
• 645403-23-2 N-adamantan-1-ylmethyl-(2-chloro-5-methoxy)-benzamide 
• 910905-39-4 2-chloro-5-methoxy-N-{2-[4-(4-methyl-piperazine-1-carbonyl)-phenylamino]-pyrimidin-5-yl}-benzamide hydrochloride 
• 1383572-79-9 C₁₅H₁₄ClNO₂ 
• 1363332-98-2 12-O-(3-(5-(2-chloro-5-methoxy-benzoylamino)-pyrimidin-2-amino)-propyl)-berbamine 
• 1363333-06-5 5-amino-2-chloropyrimidine 
• 1454838-66-4 2-chloro-5-methoxy-N-(pyridin-4-yl)benzamide 
• 100062-35-9 (2-chloro-5-methoxy-phenacyl)-malonic acid 
• 103857-60-9 4-(2-chloro-5-methoxy-phenyl)-4-oxo-butyric acid 
• 98590-29-5 2-bromo-1-(2-chloro-5-methoxyphenyl)ethan-1-one 
• 99846-94-3 2-chloro-1-(2-chloro-5-methoxy-phenyl)-ethanone 

Relevant academic research and scientific papers

Palladium-catalyzed intramolecular C-H arylation of 2-halo-: N -Boc- N -arylbenzamides for the synthesis of N-H phenanthridinones

A palladium catalyzed synthesis of N-H phenanthridinones was developed via C-H arylation. The protocol gives phenanthridinones regioselectively by one-pot reaction without deprotection. It exhibits broad substrate scope and affords targets in up to 95% yields. Importantly, it could be applied for the less reactive o-chlorobenzamides.

HETEROCYCLIC AMINO BERBAMINE DERIVATIVES, PREPARATION METHOD AND USE THEREOF

The present invention relates to a novel berbamine derivative of formula I or a pharmaceutically acceptable salt thereof, a process for preparation of the same, a pharmaceutical composition comprising said compound and its use in manufacture of an antitumor medicament.

HETEROCYCLIC AMINOBERBAMINE DERIVATIVES, THE PREPARATION PROCESS AND USE THEREOF

The present invention relates to a novel berbamine derivative of formula I or a pharmaceutically acceptable salt thereof, a process for preparation of the same, a pharmaceutical composition comprising said compound and its use in manufacture of an antitumor medicament.

A highly efficient copper-catalyzed method for the synthesis of 2-hydroxybenzamides in water

An efficient copper-catalyzed synthetic method for the preparation of 2-hydroxybenzamides is described for the first time from 2-chlorobenzamide substrates using copper iodide/1,10-phenanthroline and a base, potassium hydroxide, in neat water. By using this reaction, a series of 2-hydroxybenzamides with functional groups such as fluoro, chloro, iodo, methoxy, amide, and alcohol have been obtained in 33-96% yield. Other aromatic 2-chloroarylamides such as naphthalene, pyridine, and thiophene are found to be equally compatible to the reaction. It is proposed that the reaction proceed via formation of copper-amide complex, which may facilitate the hydroxylation in water. Overall, the first report on copper-catalyzed hydroxylation reaction in water and first catalytic route for the synthesis of 2-hydroxybenzamides is presented. Simple purification procedure and convenience of employing low-cost reagents in neat water make this method practical and economical for the synthesis of 2-hydroxybenzamides. Georg Thieme Verlag Stuttgart · New York.

Anti-selective catalytic asymmetric nitroaldol reaction via a heterobimetallic heterogeneous catalyst

Full details of an anti-selective catalytic asymmetric nitroaldol reaction promoted by a heterobimetallic catalyst comprised of Nd5O(O iPr)13, an amide-based ligand, and NaHMDS (sodium hexamethyldisilazide) are described.

POLYCYCLIC MOLECULAR COMPOUNDS

This invention relates to compounds of Formula (I), wherein A is a carboaromatic or heteroaromatic ring having one or more substituents; R6 Formula (A) is optionally substituted with one or more substituents; and n is 0, 1 or an integer greater than 1 and when n is 1 or greater the bond or bonds between the carbon atoms may be saturated or unsaturated, which bind the P2X7 receptor with high affinity. This invention also relates to methods for the diagnosis, treatment or monitoring of disorders in which the P2X7 receptor is implicated, in particular the diagnosis, treatment or monitoring of (the progression of) neuroinflammatory and neurodegenerative disorders in a subject.

Cubyl amides: Novel P2X7 receptor antagonists

Polycyclic amides 2 and 5-9 were successfully synthesised and their lipophilicity profiles were evaluated using reverse-phase HPLC. All synthesised compounds possessed P2X7R antagonistic properties when tested on rat spinal cord microglia cells. Extensive screening for binding to other neuroreceptor subtypes demonstrated their P2X7 selectivity.

Discovery of (R)-9-ethyl-1,3,4,10b-tetrahydro-7-trifluoromethylpyrazino[2, 1-a]isoindol-6(2H)-one, a selective, orally active agonist of the 5-HT 2C receptor

Robust pharmaceutical treatment of obesity has been limited by the undesirable side-effect profile of currently marketed therapies. This paper describes the synthesis and optimization of a new class of pyrazinoisoindolone- containing, selective 5-HT2C agonists as antiobesity agents. Key to optimization of the pyrazinoisoindolone core was the identification of the appropriate substitution pattern and functional groups which led to the discovery of (R)-9-ethyl-1,3,4,10b-tetrahydro-7-trifluoromethylpyrazino[2,1-a] isoindol-6(2H)-one (58), a 5-HT2C agonist with > 300-fold functional selectivity over 5-HT2B and > 70-fold functional selectivity over 5-HT2A. Oral dosing of 58 reduced food intake in an acute rat feeding model, which could be completely reversed by a selective 5-HT2C antagonist and caused a reduction in body weight gain in a 4-day rat model.

PYRIMIDINE COMPOUNDS AND METHODS OF USE

The invention provides pyrimidine compounds having formula (A): The pyrimidine compounds of the invention are capable of inhibiting kinases, such as members of the Src kinase family, and various other specific receptor and non-receptor kinases.

Diazinopyrimidines

The present invention provides a compound of the formula: or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, X1, X2, and Ar1 are as defined herein. The present invention als