Slow Release of Organoboronic Acids in Cross-coupling Reactions

A method of performing a chemical reaction includes reacting a compound selected from the group consisting of an organohalide and an organo-pseudohalide, and a protected organoboronic acid represented by formula (I) in a reaction mixture: R1-B-T; where R1 represents an organic group, T represents a conformationalIy rigid protecting group, and B represents boron having sp3 hybridization. When unprotected, the corresponding organoboronic acid is unstable by the boronic acid neat stability test. The reaction mixture further includes a base having a pKB of at least 1 and a pal ladium catalyst. The method further includes forming a cross-coupled product in the reaction mixture.

Attached files:
WO 2010036921.jpg

Patents:
WO 2,010,036,921

Inventor(s): BURKE MARTIN D [US]; KNAPP DAVID M [US]; GILLIS ERIC P [US]

Type of Offer: Licensing



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