3736-36-5

Usage

Uses

Used in Pharmaceutical Industry:
Tropine benzilate is used as a smooth muscle relaxant for its ability to alleviate muscle spasms and gastrointestinal disorders. Its anticholinergic properties help in reducing the effects of acetylcholine, leading to a relaxation of smooth muscles and relief from spasms.
Used in Neurological Treatments:
In the field of neurology, Tropine benzilate is used as an anti-neurotic agent, helping to manage symptoms associated with neurological conditions that involve overactivity of the nervous system.
Used in Gastroenterology:
Tropine benzilate is utilized for the treatment of gastrointestinal disorders, where its muscle relaxant properties can help in reducing gastrointestinal motility and alleviating symptoms such as abdominal pain and discomfort.
Used in Motion Sickness Management:
As an anticholinergic drug, Tropine benzilate is used to manage motion sickness, where its effects on the nervous system can help in reducing the symptoms of nausea and vomiting associated with motion.
Used in Parkinson's Disease Research:
Tropine benzilate is being studied for its potential use in treating Parkinson's disease. Its ability to modulate dopamine levels in the brain suggests that it could be a candidate for therapeutic intervention in this neurodegenerative condition, although further research is required to confirm its efficacy and safety in this context.

InChI:InChI=1/C22H25NO3/c1-23-19-10-11-20(23)14-16(13-19)15-6-5-9-18(12-15)22(26,21(24)25)17-7-3-2-4-8-17/h2-9,12,16,19-20,26H,10-11,13-14H2,1H3,(H,24,25)

Upstream product

• 120-29-6 3-tropanol 
• 52182-15-7 ethyl benzilate 
• 15441-11-9 Benzilic acid imidazolide 
• 76-89-1 methyl benzilate 
• 76-93-7 Benzilic acid 
• 134-81-6 benzil 

Downstream Products

• 74051-28-8 3endo-benziloyloxy-8anti-heptyl-8syn-methyl-nortropanium; bromide 
• 124136-86-3 3endo-benziloyloxy-8syn-methyl-8anti-octyl-nortropanium; bromide 
• 121970-57-8 3endo-benziloyloxy-8syn-methyl-8anti-nonyl-nortropanium; bromide 
• 120856-60-2 3endo-benziloyloxy-8anti-decyl-8syn-methyl-nortropanium; bromide 
• 120855-51-8 3endo-benziloyloxy-8syn-methyl-8anti-octyloxycarbonylmethyl-nortropanium; chloride 
• 123966-45-0 3endo-benziloyloxy-8anti-hexyloxycarbonylmethyl-8syn-methyl-nortropanium; bromide 
• 121707-49-1 3endo-benziloyloxy-8anti-heptyloxycarbonylmethyl-8syn-methyl-nortropanium; chloride 
• 21735-94-4 Tropinbenzilat-methiodid 

Relevant academic research and scientific papers

A 2 the hydroxy [...] ― 2,2 the the ― 3 α [...] diphenylgermanium acetic acid [...] (8 the [...] azabicyclo [3, 2, 1]) ― 3 the method for the preparation of octyl [...]

The invention discloses a method for preparing 2-hydroxy-2,2-diphenylacetic acid-3alpha-(8-aza-bicyclo(3,2,1))-3-trioctyl. The method comprises the following steps of: by taking dibenzoyl as a raw material, carrying out rearrangement on the raw material so as to obtain dihydroxy-phenylacetic acid; reacting dihydroxy-phenylacetic acid with dimethyl carbonate under the DBU catalysis and microwave actions so as to obtain methyl benzilate; reacting the methyl benzilate with tropine so as to obtain tropine benzilate; and carrying out N formylation and alcoholysis on the obtained tropine benzilate so as to obtain nor-tropine benzilate. Compared with the prior art, the total reaction time of the method disclosed by the invention is greatly reduced, the total yield is increased greatly, and the reaction condition is more simple, and therefore, the method is suitable for industrial production.

TROPAN COMPOUND

The conventional anticholinergic drugs for administration through inhalation have been considered to have the possibility of aggravating dysuria associated with prostatic hyperplasia mediated by blood, and it has been demanded that the conventional anticholinergic drugs for administration through inhalation will have to show reduced side effects or adverse ractions. The present invention relates to a compound represented by the general formula (I): (wherein A represents; and R1, R2, R3 and R1 each a hydrogen atom or a substituent; R5 is a substituent; X- is an anion;the symbol: denotes an exo-form or endo-form, or their mixture), its salt or solvation product thereof. They are useful as a prophylactic and/or therapeutic agent with reduced side effects or adverse reactions for the diseases mediated by the muscarinic receptor.

Synthesis, antimuscarinic activity and quantitative structure-activity relationship (QSAR) of tropinyl and piperidinyl esters

A series of tropinyl and piperidinyl esters was synthesized and evaluated for inhibitory activities on the endothelial muscarinic receptors of rat (M3) and rabbit (M2) aorta. Some of the esters (cyclohexylphenylglycolates and cyclohexylphenylpropionates) were found to be better antimuscarinic compounds than standard M2 and M3 inhibitors such as AFDX116 and 4-diphenylacetoxy-N-methylpiperidine (DAMP), with pKEC50 values in the range of 8-9. A few esters were found to be more selective M3 than M2 inhibitors, but these tended to have low activities. The hydrophobic, electronic and steric characteristics of these esters were correlated with antimuscarinic activity by using appropriate parameters representing hydrophobicity (HPLC capacity factor, log k(w), size (molecular volume) and electronic character (Taft's polar substituent constant δ and 13C chemical shift difference Δδ). Finally, 92% of the M2-inhibitory activities of the esters could be accounted for by the size and electronic character σ* of the side chain. In contrast, the M3-inhibitory activities of these esters were mainly attributed to the electronic nature (σ*, Δδ) of the side chain, with good activity being associated with electron-withdrawing groups. Visualization of the comparative molecular field analysis (CoMFA) steric and electrostatic fields provided further confirmation of the structure-activity relationship (SAR) derived from traditional quantitative structure-activity relationship (QSAR) approaches.

Synthesis of the bronchospasmolytic agent flutropium bromide and of some homologous and configuration isomeric compounds

A technically practicable synthesis of unknown N-β-fluoroalkyl-substituted benzilic acid nortropine esters, among them (8r)-8-(2-fluoroethyl)-3α-hydroxy-1αH,5αH-tropanium bromide benzilic acid ester (flutropium bromide, Ba 598 BR), and their configuration isomeric quaternary salts via benzilic acid imidazolide is described. The quaternization which takes place with sufficiently high stereoselectivity leads to configuration isomers which differ not only in their physico-chemical properties but also in their profile of pharmacological action.