Process for the preparation and isolation of atracurium besylate

Details Process for the preparation and isolation of atracurium besylate Process for the preparation and isolation of atracurium besylate

1996-02-16

1997-11-04

Morris, Patricia L.

Organic compounds -- part of the class 532-570 series

Organic compounds

Heterocyclic carbon compounds containing a hetero ring...

C07D21724

Patent

active

056841540

ABSTRACT:
A process of producing atracurium besylate that substantially reduces the level of impurities in the final product and avoids the repeated use of ether is provided. In accordance with such a process, N, N'-4,10-dioxa-3,11-dioxotridecylene-1,13-bis-tetrahydropapaverine (Compound 1), methyl benzenesulfonate and a catalytic amount of an insoluble base in a solvent are combined to form a reaction mixture that is maintained for a period of time sufficient for atracurium besylate formation. The reaction mixture is then filtered to remove the insoluble base and the atracuriurn besylate is precipitated.

REFERENCES:
patent: 4179507 (1979-12-01), Stenlake et al.
patent: 5453510 (1995-09-01), Hill et al.
Stenlake, J.B., et al., "Biodegradable neuromuscular blocking agents. Part 4. Atracurium Besylate and related polyalkylene di-esters", Eur. J. Med. Chem., 16(6):515 524 (1981).
Stenlake, J.B., et al., "Biodegradable neuromuscular blocking agents. Part 6. Stereochemical studies on atracurium and related polyalkylene di-esters", Eur. J. Med. Chem., 19(5):441-450 (1984).

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