发明名称 |
PROCESS FOR THE PREPARATION OF 2,3,4,5-TETRAHYDRO-1H-PYRIDO[4,3-B]INDOLE DERIVATIVES |
摘要 |
The value of the invention is the application of the cyclization of Schiff-bases of the general formula (3a-i), where R1 - R8 are substituents defined in example 1, whereby R9 = Cl using complex bases of amides of group I of the periodic table (NaNH2, KNH2) from 2.1 - 5 equiv. and alcoholates of group I of the periodic table (t-BuONa, tBuOK) from 0.05 - 2 equiv. with the advantage of application of 3 equiv. of NaNH2 and 0.05 equiv. of t-BuONa, or their mixtures with PEG (m.w. = 500 - 6000), or crown ethers, or catalysts of phase transfer lithium in inert proton-free diluents, such as benzene, cyclohexane, toluene, xylene, 1,2-dimethoxyethane, dioxane, etc., with the advantage of using THF, at a temperature from 20 °C to boiling point of the diluent used, or with the application of organo-metallic bases such as LDA, t-BuLi in inert proton-free diluents at a temperature from -80°C to 25 °C. |
申请公布号 |
WO2011139242(A3) |
申请公布日期 |
2012.03.15 |
申请号 |
WO2011SK00011 |
申请日期 |
2011.05.06 |
申请人 |
USTAV EXPIREMENTALNEJ FARMAKOLOGIE A TOXIKOLOGIE SAV;SNIRC, VLADIMIR;BUCHMAN, MAREK;STEFEK, MILAN;BAUER, VIKTOR;STOLC, SVORAD;MIHALOVA, DANICA;PATOPRSTY, VLADIMIR;POVAZANEC, FRANTISEK |
发明人 |
SNIRC, VLADIMIR;BUCHMAN, MAREK;STEFEK, MILAN;BAUER, VIKTOR;STOLC, SVORAD;MIHALOVA, DANICA;PATOPRSTY, VLADIMIR;POVAZANEC, FRANTISEK |
分类号 |
C07D471/04 |
主分类号 |
C07D471/04 |
代理机构 |
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代理人 |
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主权项 |
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地址 |
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