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US 6,603,013 B2Granted
Heterogeneously catalyzed process for cross coupling alkenyl halides with boronic acids
AssigneeMerck & Co., Inc.
InventorsYongkui Sun, Carl LeBlond, John R. Sowa, Jr.
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Abstract
The present invention relates to a process wherein heterogeneous finely-dispersed palladium catalysts are used in a cross-coupling reaction of alkenyl halides and aryl or heteroaryl boronic acids in the presence of base in an aprotic solvent to produce aryl- or heteroaryl-olefin compounds of Formula I:
Claims15
A process for synthesizing a compound of formula I,
- comprising reacting a boronic acid of formula II,
- with an alkenyl halide of formula III,
- wherein X, Y and Z are independently hydrogen, CF3, C1-6 alkoxy, NO2, CN, halo, C1-6 alkyl, NH2, COOH, COO(C1-6 alkyl), or N[(C1-6 alkyl]2, acetanilide, amide, C2-6 alkenyl, or aryl;
- and Q is Cl, Br, or I;
- in the presence of a heterogeneous palladium catalyst and a base in an aprotic solvent to produce a compound of formula I.
2 more elements
Dependencies are inferred from the claim text.