| 摘要 |
Benzo(b)pyrano(3,2-h)acridin-7-one derivatives (I), their isomers, N-oxides, and salts with acids and bases are new. <??>Benzo(b)pyrano(3,2-h)acridin-7-one derivatives (I), their isomers, N-oxides, and salts with acids and bases are new. <??>X, Y = H, halogen, SH, CN, NO2, 1-6C alkyl, trihaloalkyl or trihaloalkylcarbonylamino, ORa, NRaRb, -NRa-C(O)-T1, -O-T2-NRaRb, -O-T2-O-Ra, -N-Ra-T2-ORa, -NRa-T2-NRaRb, -OC(O)-T1- or -NRa-T2-COO-Ra, or when they are on adjacent positions X and Y together may form methylenedioxy or ethylenedioxy; <??>Ra, Rb = H, 1-6C alkyl, aryl, or aryl 1-6C alkyl; or <??>NRaRb = 5 or 6 membered heterocycle which may contain O or N as a second heteroatom; <??>T1 = 1-6C alkyl, 2-6C alkenyl, aryl, aryl-1-6C alkyl, 1-6C alkylene substituted by ORa or NRaRb; <??>T2 = 1-6C alkylene; <??>R1 = H or 1-6C alkyl; <??>R2 = H, 1-6C alkyl, ORa, NRaRb, -NRa-C(O)-T1, -O-T2-NRaRb, -O-T2-O-Ra, -N-Ra-T2-ORa, -NRa-T2-NRaRb, -OC(O)-T1- or -NRa-T2-COO-Ra; <??>R3, R4 = H or 1-6C alkyl; <??>W = -CH(R5)-CH(R6)-, -CH=C(R7)-, -C(R7)=CH-, or -C(O)-CH(R8)-; <??>R5, R6 = A1 or A2; <??>A1 = -W1-C(W2)-W3-T1, -W4-C(W2)-T1, -W1-S(O)n-W3-T1, or -W1-S(O)n-T1; <??>A2 = H, OH, 1-6C alkoxy, alkylcarbonyloxy, arylcarbonyloxy, arylalkyl carbonyloxy, or amino (optionally substituted by one or two 1-6C alkyl groups); <??>W1, W3 = O, S, or N substituted by H, alkyl, aryl, or aralkyl; <??>W2 = O or S; <??>W4 = S or N substituted by H, alkyl, aryl, or aralkyl; <??>n = 1 or 2; <??>R7 = OH, 1-6C alkoxy, -C(W2)-T1, -W1-C(W2)-W3-T1, -W1-C(W2)-T1, -W1-S(O)n-W3-T1, -W1-S(O)n-T1 or H; and <??>R8 = 1-6C alkoxy, alkylcarbonyloxy or OH. <??>Provided that: <??>(1) either R5 and R6 are both A1, or one is A1 and the other is A2; <??>(2) R7 is only H when R2 is -O-T2-ORa and/or X is H and Y is in position 13 of the naphthyl system in the pentacyclic skeleton and is amino optionally substituted by alkyl, acyl, or trihaloalkylcarbonyl; and <??>(3) R8 is only OH when R2 is -O-T2-ORa. <??>An Independent claim is also included for the preparation of (I).
|
