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A versatile route to potential dihydrofolate reductase inhibitors via the hitherto unknown 6‐benzyl‐2‐( O ‐methyl)uracils: Synthesis of isotrimethoprim
Author(s) -
Botta Maurizio,
Artico Marino,
Massa Silvio,
Gambacorta Augusto
Publication year - 1989
Publication title -
journal of heterocyclic chemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.321
H-Index - 59
eISSN - 1943-5193
pISSN - 0022-152X
DOI - 10.1002/jhet.5570260372
Subject(s) - chemistry , dihydrofolate reductase , uracil , pyrimidine , derivative (finance) , stereochemistry , combinatorial chemistry , organic chemistry , biochemistry , enzyme , dna , financial economics , economics
The synthesis of 2, 4‐diamino‐6‐(3, 4, 5‐trimethoxybenzyl)pyrimidine (isotrimethoprim) has been accomplished starting from 2‐( O ‐methyl)‐6‐(3, 4, 5‐trimethoxybenzyl)uracil by standard procedures. The benzyluracil derivative has been obtained by reacting O ‐methylisourea sulphate and ethyl 3, 4, 5‐trimethoxyphenacetylace‐tate.