- Synthesis of bicyclic aza-enones via a lewis acid catalysed Michael-type addition with silyl enol ethers bearing a nitrogen atom
-
Silyl enol ethers bearing a nitrogen atom protected by an electron-withdrawing group give in high yield a Micheal-type addition with hemiacetal vinylog or a mixture of methyl vinyl ketone and an alcohol in the presence of boron trifluoride etherate as a catalyst. The aza-1,5-diketones so prepared can be cyclised leading to aza-enones precursors of some biologycally active structures.
- Duhamel, Pierre,Deyine, Abdallah,Poirier, Jean-Marie
-
p. 3863 - 3866
(2007/10/02)
-
- 1,4-Benzodiazepine derivatives
-
1,4-Benzodiazepine derivatives of the formula: STR1 (in which R1 is pyrrolidinyl or piperidinyl each optionally substituted by C1-3 alkyl, phenyl-C1-3 alkyl, C1-5 alkanoyl, or C2-5 alkoxycarbonyl, R2 is hydrogen, hydroxy, or acetoxy, R3 is C1-3 alkyl, phenyl-C1-3 alkyl, or phenyl optionally substituted by one or two halogens, X is hydrogen, halogen, C1-3 alkyl, C1-3 alkoxy, nitro, trifluoromethyl, or di-C1-3 alkyl-amino, and n is 1 or 2) or pharmaceutically acceptable acid addition salts thereof, which are useful as a psychotropic agent such as anti-depressant or anxiolytic agent can be prepared from several routes.
- -
-
-