ChemInform Abstract: BIODEGRADABLE NEUROMUSCULAR BLOCKING AGENTS. PART 3. BISQUATERNARY ESTERS

Abstract

Die bisquaternären Ammoniumsalze (V) und (X) werden, wie im Schema angegeben, synthetisiert.

Alkaloids: Chemical and Biological Perspectives

“…Analysis by NMR spectrometry or, better, by HPLC, which separates the cis-cis-, cis-trans-, and trans-trans,isomers, shows that in each of the synthesized R, R, R, S/meso, and S, S products the three isomers are present in the approximate ratios 10.5 : 6.5 : 1. The molar neuromuscular-blocking potencies of the three products relativ(: to (+)-tubocurarine (= 100) determined using the gastrocnemius musclesciatic nerve preparation in anaesthetized cats are: R, R 231, R, S/meso 133, and S, S 89, again showing the considerable influence that stereochemistry has on the biological activity (504).…”

“…for a 0.3 mg/kg dose. To permit the preparation of small volume injections for clinical use, the alkylating agent finally chosen for the quaternization was methyl benzenesulphonate -the drug is put up in 2.5-or 5-ml ampoules containing 10 mg/ml and the solution is stable for at least two years at the optimal pH of 3.5 (which inhibits possible occurrence of the Hofmann elimination) and storage at 5°C (504,527,534,536).…”

Chromatographic and Molecular Simulation Study on the Chiral Recognition of Atracurium Besylate Positional Isomers on Cellulose Tri-3, 5 Dimethylphenycarbamate (CDMPC) Column and its Recognition Mechanism

“…Several methods in the form of patents have been advanced for the preparation and separation of atracurium besylate isomers. Stealake et al [16], suggested a method preparation of quaternary ammonium compounds such as Atracurium besylate, Atracurium mesylate, R-atracurium besylate but the method does not cover the aspect of getting the cisatracurium besylate. The US Patent No: 5,453,510 [17], suggests an HPLC separation method of the Isomers of Atracurium besylate but in the presence of a strong acid.…”

“…To effectively develop a chiral separation method, using a particular CSP, it is important to first understand and interpret the interaction between the enantiiomer and the chiral selector [23]. Most of the methods developed for the separation of atracurium besylate isomers are either expensive or use solvent posing problem to the column and CSP [16][17][18][19][20]. Unlike other chiral compounds, the chiral recognition and separation of atracurium besylate is cumbersome and achievable on relatively fewer CSPs and mobile phases that are pH, concentration and temperature sensitive [16][17][18][19][20][21][22].…”

“…Most of the methods developed for the separation of atracurium besylate isomers are either expensive or use solvent posing problem to the column and CSP [16][17][18][19][20]. Unlike other chiral compounds, the chiral recognition and separation of atracurium besylate is cumbersome and achievable on relatively fewer CSPs and mobile phases that are pH, concentration and temperature sensitive [16][17][18][19][20][21][22]. The choice of column, appropriate mobile phase and specific HPLC conditions do affect its recognition [16][17][18][19][20][21][22].…”