890-59-5

Upstream product

• 6298-19-7 2-chloro-3-aminopyridine 
• 89-77-0 2-Amino-4-chlorobenzoic acid 
• 5900-58-3 2-amino-4-chloro-benzoic acid methyl ester 
• 865-47-4 potassium tert-butylate 
• 41995-04-4 4-chloro-2-nitro-benzoyl chloride 
• 6280-88-2 4-chloro-2-nitro-benzoic acid 
• 1032-41-3 4-chloro-N-(2-chloro-pyridin-3-yl)-2-nitro-benzamide 

Relevant academic research and scientific papers

New pyridobenzodiazepine derivatives as potential antipsychotics: Synthesis and neurochemical study

The discovery of a new, safe, atypical antipsychotic remains an important challenge. To achieve this goal, a series of N-methylpiperazinopyrido[2,3- b][1,4]- and -[1,5]- and -pyrido[4,3-b][1,4]- and -[1,5]-benzodiazepines were synthesized. The dopaminergic (D1, D2), serotonergic (5-HT2), and cholinergic (M) affinities, frequently remarked in the action mechanisms of antipsychotic drugs, were determined using their respective in vitro receptor binding assays. All affinities were reduced for each compound. Optimal substituents were found to be in the 2- or 8-position for the retention of affinities, while substitution at the 5-position by acyl or alkyl groups dramatically diminished binding affinities. Pyridobenzodiazepine derivatives, such as clozapine, were found to be inactive or only weakly effective against apomorphine-mediated stereotypes in rats. In an original and complex behavioral model developed in dogs and successfully used to differentiate distinct classes of psychotropic drugs and to discriminate between typical and atypical neuroleptic drugs, 8-chloro-6-(4-methyl-1-piperazinyl)-11H- pyrido[2,3-b][1,4]benzodiazepine (9), 8-methyl-6-(4-methyl-1-piperazinyl)- 11H-pyrido[2,3-b][1,4]benzodiazepine (12), and 5-(4-methyl-1-piperazinyl)- 11H-pyrido[2,3-b][1,5]benzodiazepine (16) showed most of the behavioral characteristics previously described for neuroleptics. Their neurochemical profiles, particularly their 5-HT2/D2 pK(i) ratios, were compatible with an atypical antipsychotic effect. These compounds were selected for further investigation. The proposed modulations could lead to new possibilities for the pharmacochemistry of diarylazepines.

Substituted pyrido(2,3-B) (1,4) benzodiazepin-6-ones, and medicaments containing these compounds

New substituted pyrido[2,3-b][1,4]benzodiazepin-6-ones suitable as vagal pacemakers for the treatment of bradycardias and bradyarrhythmias in human and veterinary medicine are described.

Process for preparing derivatives of 5,11-dihydro-6h-pyrido[2,3-b][1,4]-benzodiazepin-6-one, and the final derivatives and synthesis intermediates obtained thereby

This invention relates to a process for preparing derivatives of 5,11-dihydro-6H-pyrido[2,3-b][1,4]-benzodiazepin-6-one of general formula (I) STR1 in which R is hydrogen, halogen or methyl; R1 and R2 are linear or branched C2/