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Tamotsu Takahashi - One of the best experts on this subject based on the ideXlab platform.

Piero Salvadori - One of the best experts on this subject based on the ideXlab platform.

  • silylation Desilylation of propargyl amides rapid synthesis of functionalised aldehydes and β lactams
    Tetrahedron, 2007
    Co-Authors: Laura Antonella Aronica, Giulia Valentini, Anna Maria Caporusso, Piero Salvadori
    Abstract:

    Abstract Propargyl functionalised β-silylalkenals were easily prepared starting from suitable propargyl compounds by a silylformylation process. In particular the use of propargyl tosyl amides allowed the synthesis of α,β-unsaturated aldehydes through a two-step sequence of silylformylation–Desilylation reactions. TBAF was employed to induce the Desilylation process that was performed under very mild experimental conditions and occurred along with an elimination step of the tosylamido moiety affording 2-methylaryl-2-alkenals with good yields and stereoselectivity. When the tosyl amides were reacted with a hydrosilane in the presence of catalytic amounts of 1,8-diazabicyclo[5.4.0]undec-7-ene (DBU) α-silylmethylene-β-lactams were synthesised through a silylcarbocyclisation process. A high chemoselectivity towards the β-lactam was observed when dialkyl propargyl amides were employed. The obtained β-lactams were easily transformed into the corresponding methylaryl-β-lactams by fluoride induced aryl migration–Desilylation with total retention of configuration of the migrating group and complete stereoselectivity towards the more stable β-lactam ( E )-isomer.

  • Silylation–Desilylation of propargyl amides: rapid synthesis of functionalised aldehydes and β-lactams
    Tetrahedron, 2007
    Co-Authors: Laura Antonella Aronica, Giulia Valentini, Anna Maria Caporusso, Piero Salvadori
    Abstract:

    Abstract Propargyl functionalised β-silylalkenals were easily prepared starting from suitable propargyl compounds by a silylformylation process. In particular the use of propargyl tosyl amides allowed the synthesis of α,β-unsaturated aldehydes through a two-step sequence of silylformylation–Desilylation reactions. TBAF was employed to induce the Desilylation process that was performed under very mild experimental conditions and occurred along with an elimination step of the tosylamido moiety affording 2-methylaryl-2-alkenals with good yields and stereoselectivity. When the tosyl amides were reacted with a hydrosilane in the presence of catalytic amounts of 1,8-diazabicyclo[5.4.0]undec-7-ene (DBU) α-silylmethylene-β-lactams were synthesised through a silylcarbocyclisation process. A high chemoselectivity towards the β-lactam was observed when dialkyl propargyl amides were employed. The obtained β-lactams were easily transformed into the corresponding methylaryl-β-lactams by fluoride induced aryl migration–Desilylation with total retention of configuration of the migrating group and complete stereoselectivity towards the more stable β-lactam ( E )-isomer.

  • silylformylation Desilylation of propargyl amides synthesis of α β unsaturated aldehydes
    Tetrahedron Letters, 2006
    Co-Authors: Laura Antonella Aronica, Giulia Valentini, Anna Maria Caporusso, Patrizio Raffa, Piero Salvadori
    Abstract:

    Abstract α,β-Unsaturated aldehydes are prepared from easily available propargyl amides through a two-step sequence of silylformylation–Desilylation reactions. The substituent on the nitrogen atom markedly influences both reactions, β-silylalkenals being formed in the presence of tosyl or tert -butoxycarbonyl protected amines. TBAF is employed to induce the Desilylation process that is performed under very mild experimental conditions. A contemporary elimination step occurs when tosylamido aldehydes are reacted affording 2-methylaryl-2-alkenals, while this process can be suppressed changing the functional group to NBOC, thus allowing the formation of β-amino carbonyl compounds.

  • Silylformylation–Desilylation of propargyl amides: synthesis of α,β-unsaturated aldehydes
    Tetrahedron Letters, 2006
    Co-Authors: Laura Antonella Aronica, Giulia Valentini, Anna Maria Caporusso, Patrizio Raffa, Piero Salvadori
    Abstract:

    Abstract α,β-Unsaturated aldehydes are prepared from easily available propargyl amides through a two-step sequence of silylformylation–Desilylation reactions. The substituent on the nitrogen atom markedly influences both reactions, β-silylalkenals being formed in the presence of tosyl or tert -butoxycarbonyl protected amines. TBAF is employed to induce the Desilylation process that is performed under very mild experimental conditions. A contemporary elimination step occurs when tosylamido aldehydes are reacted affording 2-methylaryl-2-alkenals, while this process can be suppressed changing the functional group to NBOC, thus allowing the formation of β-amino carbonyl compounds.

Xiaozhong Liu - One of the best experts on this subject based on the ideXlab platform.

Geert-jan Boons - One of the best experts on this subject based on the ideXlab platform.

Laura Antonella Aronica - One of the best experts on this subject based on the ideXlab platform.

  • silylation Desilylation of propargyl amides rapid synthesis of functionalised aldehydes and β lactams
    Tetrahedron, 2007
    Co-Authors: Laura Antonella Aronica, Giulia Valentini, Anna Maria Caporusso, Piero Salvadori
    Abstract:

    Abstract Propargyl functionalised β-silylalkenals were easily prepared starting from suitable propargyl compounds by a silylformylation process. In particular the use of propargyl tosyl amides allowed the synthesis of α,β-unsaturated aldehydes through a two-step sequence of silylformylation–Desilylation reactions. TBAF was employed to induce the Desilylation process that was performed under very mild experimental conditions and occurred along with an elimination step of the tosylamido moiety affording 2-methylaryl-2-alkenals with good yields and stereoselectivity. When the tosyl amides were reacted with a hydrosilane in the presence of catalytic amounts of 1,8-diazabicyclo[5.4.0]undec-7-ene (DBU) α-silylmethylene-β-lactams were synthesised through a silylcarbocyclisation process. A high chemoselectivity towards the β-lactam was observed when dialkyl propargyl amides were employed. The obtained β-lactams were easily transformed into the corresponding methylaryl-β-lactams by fluoride induced aryl migration–Desilylation with total retention of configuration of the migrating group and complete stereoselectivity towards the more stable β-lactam ( E )-isomer.

  • Silylation–Desilylation of propargyl amides: rapid synthesis of functionalised aldehydes and β-lactams
    Tetrahedron, 2007
    Co-Authors: Laura Antonella Aronica, Giulia Valentini, Anna Maria Caporusso, Piero Salvadori
    Abstract:

    Abstract Propargyl functionalised β-silylalkenals were easily prepared starting from suitable propargyl compounds by a silylformylation process. In particular the use of propargyl tosyl amides allowed the synthesis of α,β-unsaturated aldehydes through a two-step sequence of silylformylation–Desilylation reactions. TBAF was employed to induce the Desilylation process that was performed under very mild experimental conditions and occurred along with an elimination step of the tosylamido moiety affording 2-methylaryl-2-alkenals with good yields and stereoselectivity. When the tosyl amides were reacted with a hydrosilane in the presence of catalytic amounts of 1,8-diazabicyclo[5.4.0]undec-7-ene (DBU) α-silylmethylene-β-lactams were synthesised through a silylcarbocyclisation process. A high chemoselectivity towards the β-lactam was observed when dialkyl propargyl amides were employed. The obtained β-lactams were easily transformed into the corresponding methylaryl-β-lactams by fluoride induced aryl migration–Desilylation with total retention of configuration of the migrating group and complete stereoselectivity towards the more stable β-lactam ( E )-isomer.

  • silylformylation Desilylation of propargyl amides synthesis of α β unsaturated aldehydes
    Tetrahedron Letters, 2006
    Co-Authors: Laura Antonella Aronica, Giulia Valentini, Anna Maria Caporusso, Patrizio Raffa, Piero Salvadori
    Abstract:

    Abstract α,β-Unsaturated aldehydes are prepared from easily available propargyl amides through a two-step sequence of silylformylation–Desilylation reactions. The substituent on the nitrogen atom markedly influences both reactions, β-silylalkenals being formed in the presence of tosyl or tert -butoxycarbonyl protected amines. TBAF is employed to induce the Desilylation process that is performed under very mild experimental conditions. A contemporary elimination step occurs when tosylamido aldehydes are reacted affording 2-methylaryl-2-alkenals, while this process can be suppressed changing the functional group to NBOC, thus allowing the formation of β-amino carbonyl compounds.

  • Silylformylation–Desilylation of propargyl amides: synthesis of α,β-unsaturated aldehydes
    Tetrahedron Letters, 2006
    Co-Authors: Laura Antonella Aronica, Giulia Valentini, Anna Maria Caporusso, Patrizio Raffa, Piero Salvadori
    Abstract:

    Abstract α,β-Unsaturated aldehydes are prepared from easily available propargyl amides through a two-step sequence of silylformylation–Desilylation reactions. The substituent on the nitrogen atom markedly influences both reactions, β-silylalkenals being formed in the presence of tosyl or tert -butoxycarbonyl protected amines. TBAF is employed to induce the Desilylation process that is performed under very mild experimental conditions. A contemporary elimination step occurs when tosylamido aldehydes are reacted affording 2-methylaryl-2-alkenals, while this process can be suppressed changing the functional group to NBOC, thus allowing the formation of β-amino carbonyl compounds.