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US 2004/0006243 A1Published application
Method of producing oxybutynin and its derivatives
AssigneeThe University of Tokyo
InventorsMasakatsu Shibasaki, Motomu Kanai
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Abstract
An oxybutynin and its derivatives are produced by reacting a phenylketone with a silylcyanide in the presence of a specified asymmetric catalyst to obtain a siloxynitrile, and then reacting the siloxynitrile with a reducing agent and oxidizing the resulting aldehyde, or subjecting the siloxynitrile to a hydrolysis.
Claims8
A method of producing an oxybutynin and its derivatives, which comprises reacting a phenylketone with a silylcyanide in the presence of an asymmetric catalyst formed by bonding a metal to a catechol portion of a ligand represented by the following general formula (I):
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- (wherein each of R1, R2 and R3 is a substituent on an aromatic ring, and R4 is a hydrogen atom or an electron attractive group, provided that a ring-closing structure may be formed by two R4, and R5 is a methyl group, a methoxy group, a dimethyl amino group or an electron attractive group, and X is P or As, and n is 1 to 3) to form a siloxynitrile, and then reacting the siloxynitrile with a reducing agent to obtain an aldehyde and oxidizing the aldehyde, or subjecting the siloxynitrile to a hydrolysis.
Dependencies are inferred from the claim text.