Synthesis of aminoarylboronic esters and substituted...

Organic compounds -- part of the class 532-570 series – Organic compounds – Boron containing

Reexamination Certificate

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Reexamination Certificate

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06958420

ABSTRACT:
A process is described for synthesizing aminoarylboronic esters of the general formulawherein R, R2, and R3are each an alkyl, aryl, vinyl, alkoxy, carboxylic esters, amides, or halogen; Ar is any variety of phenyl, naphthyl, anthracyl, heteroaryl; and R1is alkyl, hydrogen, or aryl. The aminoarylboronic esters are produced via the metal-catalyzed coupling of arylboronic esters of the general formulawherein R and R1are any non-interfering group and X is chloro, bromo, iodo, triflates, or nonaflates to amines (primary and secondary). In particular, a process is described for the synthesis of the aminoarylboronic esters via a step-wise or tandem process in which one catalytic event is a metal-catalyzed borylation and the other catalytic event is a metal-catalyzed amination.

REFERENCES:
patent: WO 2000015213 (2000-03-01), None
patent: WO 2000077001 (2000-12-01), None
patent: WO 2001010868 (2001-02-01), None
patent: WO 2001097786 (2001-12-01), None
Staab.Heinx A. et al Justus Liebigs Annalen de Chemie (1971), 753, 80-91.
Klis, Tomasz et al , Main Group Metal Chemistry (20020 25 (8), 479-484.

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