Process for the preparation of Montelukast

Details Process for the preparation of Montelukast Process for the preparation of Montelukast

2006-02-03

2008-08-26

Dentz, Bernard (Department: 1625)

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

Organic compounds

Heterocyclic carbon compounds containing a hetero ring...

Reexamination Certificate

active

07417149

ABSTRACT:
The present invention relates to a process for the preparation of Montelukast and the salts thereof comprising the following steps:(a) reaction of a compound Awith a compound A2in which n varies between 1 and 2 and, when n is 1, R is methyl and, when n is 2, R is a C1-C4alkyl or an aryl, and X is a leaving group, by nucleophilic substitution reactions in dipolar organic solvents to yield the compound A3(b) reaction of the compound A3 with an inorganic acid HY, in which Y is Cl, Br, I, and subsequent isolation of the resultant salt A4;(c) optional conversion of the salt A4 into the compound A3;(d) methylation of the salt A4 and/or of the compound A3 to yield Montelukast.

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Dufresne et al., Synthesis of Montelukast (MK-0476) Metabolic Oxydation Products, J. Org. Chem., 1996, 61, 8518-8525.
Wang, D., et al; “Process for the preparation of montelukast sodium and its intermediate”;Caplus; 2001, 6 pages; XP-002343618.
King, A.O., et al; “An Efficient Synthesis of LTD Antagonist L-699,392”;J. Org. Chem.; 1993, vol. 58; pp. 3731-3735.

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