Organic compounds -- part of the class 532-570 series – Organic compounds – Four or more ring nitrogens in the bicyclo ring system
Patent
1978-07-19
1980-09-23
Daus, Donald G.
Organic compounds -- part of the class 532-570 series
Organic compounds
Four or more ring nitrogens in the bicyclo ring system
544260, 424250, A61K 31495, C07D48704
Patent
active
042244463
ABSTRACT:
Process for the production of methotrexate, which is N[p-([(2,4-diamino-6-pteridyl)-methyl]-N.sup.10 -methylamino)-benzoyl]-L-glutamic acid. The process includes converting 1,1-dichloroacetone with 2,4,5,6-tetraaminopyrimidine in the presence of sodium bisulfite at a constant pH between 3.5 and 5 and at a temperature between 10.degree. and 100.degree. C. The resultant 2,4-diamino-6-methylpteridine is converted in a reaction medium with bromide. 0.3 to 1.0 ml of bromine is used per 1.0 g of the 2,4-diamino-6-methylpteridine. The 2,4-diamino-6-bromo methyl pteridine is converted with p-(N-methyl)-aminobenzoyl-L-glutamic acid or a salt thereof in a polar reaction medium into methoxtrexate.
REFERENCES:
patent: 3989703 (1976-11-01), Duvaz
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Adamson, R., et al., "Arch. Int. Pharmacodyn," 1965, 153, No. 1-2, p. 87.
Daus Donald G.
Jones L.
Lonza Ltd.
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