Protected tyrosine derivatives, method for the production...

Details Protected tyrosine derivatives, method for the production... Protected tyrosine derivatives, method for the production...

2005-07-19

2005-07-19

Tsang, Cecilia J. (Department: 1625)

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

Organic compounds

Carboxylic acid esters

Reexamination Certificate

active

06919475

ABSTRACT:
The compound O-(2-[18F]fluoroethyl)-L-tyrosine has proven to be particularly suitable for positron emission tomography and has already been tested in clinical practice. Until now, the compound has been prepared according to a relatively laborious method (Wester H. J. et al., J. Nucl. Med. 1999; 40: 205-212).The invention relates to L-tyrosine derivatives of the formula (1)whereby R1represents a suitable protective group for the carboxy group, R2a suitable protective group for the amino group and R3a suitable leaving group,R1represents a methylthiomethyl group, a tetrahydrofuranyl group, a diphenylmethyl group, a para-methoxybenzyl group, a piperonyl group or a tert-butyl group, R2an alkyl- or an arylalkyl group and R3a p-tosyloxy, methanesulfonyloxy, trifluoromethanesulfonyloxy or bromine.The invention also relates to a method for preparing O-(2-[18F]-fluoroethyl)-L-tyrosine from the initial compounds of formula (1) and method for the preparation of these initial compounds.

REFERENCES:
patent: 5885548 (1999-03-01), Maier et al.
Webster et al, Journal of Nuclear Medicine, (1999) 40(1) pp205-212.

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