Organic compounds -- part of the class 532-570 series – Organic compounds – Amino nitrogen containing
Reexamination Certificate
2006-12-11
2008-11-04
Barts, Samuel A (Department: 1621)
Organic compounds -- part of the class 532-570 series
Organic compounds
Amino nitrogen containing
Reexamination Certificate
active
07446227
ABSTRACT:
A process for preparation of protriptyline hydrochloride from 5-dihydrobenzocycloheptatriene of formula (1) by coupling with chloropropyl alcohol in the presence of excess n-butyl Lithium in tetrahydrofuran under inert atmosphere, followed by preparation of mesylate derivative of formula (3) and finally the nucleophilic displacement of the mesylate group by reacting methylamine solution in methanol to give protriptyline free base of the formula (4). Also the present process reveals the hydrochloride salt formation and purification of the same to give pure pharmaceutical grade protriptyline hydrochloride with impurities less than 0.1% w/w.
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Caporusso et al, Stereoselective Synthesis of Chiral 3-Aryl-1-alkynes from Bromoalienes and heterocuprates, 2006, Published on Web (Sep. 2, 2006), J. Org. Chem., vol. 71, pp. 1902-1910, especially p 1907, para. D.
Kovi Ravishanker
Nampalli Satyam
Patel Brijesh
Tharial Peter Xavier
Apicore, LLC
Barts Samuel A
Gibson Timothy X.
Kaplan Gilman Gibson & Dernier LLP
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