US 7,579,461 B2
Processes for the preparation of rocuronium bromide and intermediates thereof
Eliezer Adar, Omer (Israel); David Sondack, Arad (Israel); Oded Friedman, Talmey Yechiel (Israel); Iosef Manascu, Omer (Israel); Tamir Fizitzki, Beer-Sheva (Israel); Boris Freger, Beer Sheva (Israel); Oded Arad, Rechovot (Israel); Alexander Weisman, Kiryat-Ekron (Israel); and Joseph Kaspi, Givatayim (Israel)
Assigned to Chemagis Ltd., Bnei Brak (Israel)
Filed on Jan. 13, 2005, as Appl. No. 11/34,510.
Claims priority of provisional application 60/536524, filed on Jan. 15, 2004.
Prior Publication US 2005/0159398 A1, Jul. 21, 2005
Int. Cl. C07J 43/00 (2006.01)
U.S. Cl. 540—96 28 Claims
 
1. A process of preparing a compound having Formula I:

OG Complex Work Unit Drawing
the process comprising:
reacting a compound having Formula II:

OG Complex Work Unit Drawing
with a molar excess of an acetylating agent, to thereby obtain a reaction mixture including a compound having Formula III:

OG Complex Work Unit Drawing
and
contacting said reaction mixture with an aqueous solution of an acid, to thereby selectively deacetylate an acetoxy group at position 3 of said compound having Formula III, thereby obtaining the compound having Formula I.