Folic acid derivatives and process for preparation

Details Folic acid derivatives and process for preparation Folic acid derivatives and process for preparation

C - Chemistry, Metallurgy

07

D

260/242.1

C07D 475/00 (2006.01)

Patent

CA 1176249

ABSTRACT A process for the preparation of a composition having the formula: Image wherein R represents hydrogen, lower alkyl, formyl or imino- methyl; R' and R" individually represent lower alkyl, hydroxyl, halo, amino or acetamido; R''' represents H or lower alkyl; m has a value of 1, 3 or 4; n has a value of zero or 1; and X is an amino acid or des-carboxy amino acid moiety selected from the group consisting of: Image Image Image Image Image and Image wherein Z is hydrogen or lower alkyl, which comprises protect- ing the corresponding pteroic acid (X=OH) at N10(R'''=H), re- acting with an acyl halide to form a mixed anhydride, react- ing with HX wherein X is an amino acid moiety of a des-carboxy amino acid moiety as defined above, and hydrolyzing to pro- vide the composition. The latter is useful as an intermediate in the preparation of radioiodinated compositions to be used in competitive protein binding and radioimmune-assays of folate compounds.

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