Process for production of heterodimers of glutamic acid
AssigneeMolecular Insight Pharmaceuticlas, Inc.
InventorsJohn W. Babich, Craig Zimmerman, Kevin P. Maresca
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Abstract
A manufacturing process for the preparation of radiolabeled compounds of formula (I) includes reacting compounds of formula (II) with a source of radionuclide of a halogen in the presence of an oxidant under acidic condition, wherein: *I is 123I, 124I, 125I or 131I; R is lower alkyl, optionally substituted with one or more fluorine atoms; Q is C(O), O, NR′, S, S(O)2, C(O)2, (CH2)p; Y is C(O), O, NR′, S, S(O)2, C(O)2, (CH2)p; R′ is H, C(O), S(O)2, C(O)2; Z is H, C1-C4 alkyl, benzyl, substituted benzyl or trialkylsilyl; m is 0, 1, 2, 3, 4 or 5; n is 0, 1, 2, 3, 4, 5 or 6; and p is 0, 1, 2, 3, 4, 5 or 6.
Claims28
A process for the preparation of a radiolabeled compound of formula (I)
- the process comprising:
- reacting a compound of formula (II) with a metal salt of *I in the presence of an oxidant under acidic conditions,
- wherein
- *I is 123I, 124I, 125I or 131I;
- R is lower alkyl, optionally substituted with one or more fluorides;
- Q is C(O), O, NR′, S, S(O)2, C(O)2, (CH2)p;
- Y is O, NR′, S, S(O)2, C(O)2, (CH2)p;
- R′ is H, C(O), S(O)2, C(O)2;
- Z is H, C1-C4 alkyl, benzyl, substituted benzyl or trialkylsilyl;
- m is 0, 1, 2, 3, 4 or 5;
- n is 0, 1, 2, 3, 4, 5 or 6;
- and
- p is 0, 1, 2, 3, 4, 5 or 6.
A process for the preparation of a radiolabeled compound of formula:
- the process comprising:
- reacting a compound of formula
- with a metal salt of *I in the presence of an oxidant under acidic conditions,
- wherein:
- *I is 123I;
- 124I;
- 125I or 131I;
- R is lower alkyl, optionally substituted with one or more fluorides;
- and
- Z is H, C1-C4 alkyl, benzyl, substituted benzyl or trialkylsilyl.
Dependencies are inferred from the claim text.