Abstract
An improved economical and eco friendly process for the enantioselective resolution of methylphenidate free base to give (2R,2’R)-(+)-threo- methylphenidate via diastereomeric salt preparation with (+)-di-para-toluyl-D-tartaric acid has been achieved. The racemic resolution performed under mild and neutral conditions having simple unit operation making process feasible for large scale production of dexmethylphenidate hydrochloride.
References
Vikram khetani, US Patent No. 6,359,139 B1, Mar.19, 2002.
Keating Gillian M, Figgitt David P, (2002) Drugs 62(13): 1899-904.
Heal David J, Pierce David M.(2006) CNS Drugs20(9): 713-738.
Perel, J; Dayton, P. Methylphenidate; Marcel decker: New York, 1976.
Maxwell, R.A.; Chaplin, E.; Eckhardt, S.B.; Soares, J.R.;Hite,(1970)J.Pharmacol. Exp. Ther.173: 158-165.
Alexei Kalinin etal; World Patent Application No. WO 2008/125914 A2.
S Ramaswamy, V Khetani, US Patent No. 5,965,734,1999.
Patrick, K.S; Caldwell, R.W; Ferris, R.M; Breese, G.R.(1987) J. Pharmacol. Exp. Ther. 241: 152-158.
Mahavir Prasad, Bin Hu, Oljan Repic, Thomas J. Blacklock, Peter Giannousis,(2000)Org process Res & Dev. 4: 55-59.
Prasad M.; Har D.; Repic O.; Blacklock T.J.; Giannousis.(1998) Tetrahedron:Aymmetry,9(12): 2133- 2136.
M. Prashad et al. (1999) Tetrahedron: Asymmetry10: 3111–3116.
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