SUBSTITUTED 1-AMINOPHTHALAZINE DERIVATIVES, PREPARATION THEREOF AND THERAPEUTIC APPLICATION THEREOF
申请人:AUGEREAU Jean Michel
公开号:US20090124624A1
公开(公告)日:2009-05-14
The invention concerns 1-amino-phthalazine derivatives of general formula (I):
Wherein A, B, L, R, R
1
, R
2
, R
3
, R
4
, R
5
and R
7
are as defined herein. The invention also concerns the preparation of said compounds and their therapeutic use.
The invention provides compounds of formula la, lb and Ic: [Formula Ia, Ib, and Ic] and salts thereof, wherein variables are as described in the specification, as well as compositions comprising a compound of formula Ia-Ic, methods of making such compounds, and methods of using such compounds, e.g., as inhibitors of bacterial RNA polymerase and as antibacterial agents.
An electrochemical methodology for the construction of α-CF3-substituted carbonylcompounds in moderate to good yields under exogenous metal and oxidant-free conditions has been developed. The protocol involves the single-electron oxidation of the aryl ring to generate a radical cation followed by a three-electron SN2 reaction resulting in the formation of α-CF3 substituted ketones.