5 research outputs found
Cobalt-Catalyzed Selective Synthesis of Isoquinolines Using Picolinamide as a Traceless Directing Group
Picolinamide
has first been employed as a traceless directing group
for the cobalt-catalyzed oxidative annulation of benzylamides with
alkynes to synthesize isoquinolines through CāH/NāH
bonds activation. Oxygen is
used as a terminal oxidant. This protocol exhibits good functional
group tolerance and excellent regioselectivity. Both terminal and
internal alkynes can be efficiently applied to this catalytic system
as substrates
Cobalt-Catalyzed Selective Synthesis of Isoquinolines Using Picolinamide as a Traceless Directing Group
Picolinamide
has first been employed as a traceless directing group
for the cobalt-catalyzed oxidative annulation of benzylamides with
alkynes to synthesize isoquinolines through CāH/NāH
bonds activation. Oxygen is
used as a terminal oxidant. This protocol exhibits good functional
group tolerance and excellent regioselectivity. Both terminal and
internal alkynes can be efficiently applied to this catalytic system
as substrates
Cobalt-Catalyzed Selective Synthesis of Isoquinolines Using Picolinamide as a Traceless Directing Group
Picolinamide
has first been employed as a traceless directing group
for the cobalt-catalyzed oxidative annulation of benzylamides with
alkynes to synthesize isoquinolines through CāH/NāH
bonds activation. Oxygen is
used as a terminal oxidant. This protocol exhibits good functional
group tolerance and excellent regioselectivity. Both terminal and
internal alkynes can be efficiently applied to this catalytic system
as substrates
One-Pot Regiospecific Synthesis of Quinoxalines via a CH<sub>2</sub>āExtrusion Reaction
A convenient
āone-potā regiospecific synthesis of
substituted quinoxalines from <i>o</i>-phenylenediamines
and ynones under metal-free conditions has been developed. An intermolecular
Michael addition reaction, a dehydration condensation, and a base-promoted
C-Ī±-CH<sub>2</sub>-extrusion were involved in this procedure,
which features high regioselectivity, efficiency, and environmental
friendliness. Various quinoxalines were provided in up to 95% yield
for 33 examples
Drug Effect Prediction by Polypharmacology-Based Interaction Profiling
Most drugs exert their effects via multitarget interactions, as hypothesized by polypharmacology. While these multitarget interactions are responsible for the clinical effect profiles of drugs, current methods have failed to uncover the complex relationships between them. Here, we introduce an approach which is able to relate complex drugāprotein interaction profiles with effect profiles. Structural data and registered effect profiles of all small-molecule drugs were collected, and interactions to a series of nontarget protein binding sites of each drug were calculated. Statistical analyses confirmed a close relationship between the studied 177 major effect categories and interaction profiles of ca. 1200 FDA-approved small-molecule drugs. On the basis of this relationship, the effect profiles of drugs were revealed in their entirety, and hitherto uncovered effects could be predicted in a systematic manner. Our results show that the prediction power is independent of the composition of the protein set used for interaction profile generation