One-step Heck Reaction Generates Nonimmunosuppressive FK506 Analogs for Pharmacological BMP Activation

Hydroamination/Heck reaction sequence for a highly regioselective one-pot synthesis of indoles using 2-chloroaniline.

A one-pot indole synthesis consisting of a highly regioselective TiCl(4)-catalyzed hydroamination and a 5-endo Heck cyclization starting from 2-chloroaniline is described, using an in-situ generated, sterically hindered imidazol-2-ylidene palladium complex.

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Mechanisms of the Mizoroki–Heck Reaction

The palladium-catalysed Mizoroki–Heck reaction is the most efficient route for the vinylation of aryl/vinyl halides or triflates. This reaction, in which a C C bond is formed, proceeds in the presence of a base (Scheme 1.1) [1, 2]. Nonconjugated alkenes are formed in reactions involving cyclic alkenes (Scheme 1.2) [1e, 2a,c,e,g] or in intramolecular reactions (Scheme 1.3) [2b,d–g] with creation...

One-pot synthesis of 4-methylisoquinolines via a sequential Pd-catalyzed Heck reaction and intramolecular cyclization.

An efficient, one-pot synthesis of 4-methylisoquinolines via a cascade Pd-catalyzed Heck reaction, intramolecular cyclization and isomerization has been developed. This reaction has a wide range of substrates with various functional groups, and the corresponding products have been obtained in good yields.

Highly active catalysts of bisphosphine oxides for asymmetric Heck reaction.

Bisphosphine oxides formed highly active asymmetric Heck catalysts, which were applied in asymmetric synthesis of pharmacologically active azacycles. Olefin insertion proceeded via cis pathways, different from P,N-ligands.