The cyclocondensation of EtO2CCH2CONRR1 (R = R1 = Me, Et; R = Me, R1 = Et; NRR1 = piperidino, pyrrolidino) and phenols I (R2 = H, Me, Me2CH; R3 = H, Me, Cl; R4 = H, Me, Me2N; R3R4 = CH2CH2CH2; R5 = H, Me2CH) in the presence of POCl5 gave chromones II (17 compds.) and III, possessing pharmacol. activities. Pharmacol. screening showed that the compds. markedly affected the central nervous system. Decreased activity was shown by compds. II with substituents at R3, R4, and R5. II (R = R1 = Me, R2 = R4 = R5 = H, R3 = Me) and III have weak anticonvulsant effects.
[Chemical and pharmacologic study on pyran derivatives. IX. Synthesis of 2-dialkylaminochromones].
BALBI, ALESSANDRO;DI BRACCIO, MARIO;
1977-01-01
Abstract
The cyclocondensation of EtO2CCH2CONRR1 (R = R1 = Me, Et; R = Me, R1 = Et; NRR1 = piperidino, pyrrolidino) and phenols I (R2 = H, Me, Me2CH; R3 = H, Me, Cl; R4 = H, Me, Me2N; R3R4 = CH2CH2CH2; R5 = H, Me2CH) in the presence of POCl5 gave chromones II (17 compds.) and III, possessing pharmacol. activities. Pharmacol. screening showed that the compds. markedly affected the central nervous system. Decreased activity was shown by compds. II with substituents at R3, R4, and R5. II (R = R1 = Me, R2 = R4 = R5 = H, R3 = Me) and III have weak anticonvulsant effects.
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