Separation of triphenylphosphine oxide from methotrexate ester a

Details Separation of triphenylphosphine oxide from methotrexate ester a Separation of triphenylphosphine oxide from methotrexate ester a

1981-12-11

1983-12-20

Coughlan, Jr., Paul M.

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

Organic compounds

Plural nitrogens bonded directly to the pteridine ring system

C07D47508

Patent

active

044219130

ABSTRACT:
An improvement in the production of methotrexate as set out in Ellard U.S. Pat. No. 4,080,325. It has been found that magnesium oxide facilitates the coupling reaction by acting as an acid acceptor. The dense grade of magnesium oxide is preferred in molar proportions of 2 to 4 moles of magnesium oxide per mole of 2,4-diamino-6-hydroxymethylpteridine. Further, the triphenylphosphine oxide which is generated by hydrolysis of the protecting groups is removed from the reaction stream by utilization of toluene or BTX-type solvents.

REFERENCES:
patent: 4079056 (1978-03-01), Piper et al.
patent: 4080325 (1978-03-01), Ellard

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