A rapid and mild esterification method using carboxylic 2,4,6-trichlorobenzoic anhydrides in the presence of 4-dimethylaminopyridine was developed. The method was also successfully applied to the synthesis of large-ring lactones, including DL-2,4,6-tridemethyl-3-deoxymethynolide.

A rapid esterification by means of mixed anhydride and its application to large-ring lactonization.

IT IS the purpose of this paper to record the results of clinical and hematologic studies on 5 children with acute leukemia treated by the intramuscular injection of a synthetic compound, 4-aminopteroylglutamic acid (aminopterin). This substance is an antagonist to folic acid regarding the growth of Streptococcus faecalis R. The occurrence of what he interpreted as an "acceleration phenomenon" in the leukemic process as seen in the marrow and viscera of children with acute leukemia treated by the injection of folic acid conjugates1 — pteroyltriglutamic acid (teropterin) and pteroyldiglutamic acid (diopterin) — and an experience gained from studies on folic . . .

https://www.nejm.org/doi/pdf/10.1056/NEJM194806032382301

Temporary remissions in acute leukemia in children produced by folic acid antagonist, 4-aminopteroyl-glutamic acid.

Molecular recognition of protein-ligand complexes : applications to drug design

Folic acid: nutritional biochemistry, molecular biology, and role in disease processes.

Research on antimetabolites of nucleic acid purines led to drugs for the treatment of acute leukemia (6-mercaptopurine and thioguanine), gout and hyperuricemia (allopurinol), and herpesvirus infections (acyclovir), and for the prevention of organ transplant rejection (azathioprine).

https://science.sciencemag.org/content/sci/244/4900/41.full.pdf

The purine path to chemotherapy

Analogs of Pteroylglutamic Acid. III. 4-Amino Derivatives

http://science.sciencemag.org/content/sci/103/2683/667.full.pdf

The Structure and Synthesis of the Liver L. casei Factor.

https://science.sciencemag.org/content/sci/102/2644/227.full.pdf

James M. Smith

Papers

Analogs of Pteroylglutamic Acid. III. 4-Amino Derivatives

The Structure and Synthesis of the Liver L. casei Factor.

Synthesis of a compound identical with the l. casei factor isolated from liver

Antagonist for pteroylglutamic acid.

Chemistry of Leucovorin