C07C37/62

Fluorination method

The present invention relates to a process for producing an organic compound comprising an .sup.18F atom. The compounds comprising an .sup.18F can be useful as PET ligands for use in diagnostics and/or scanning. The process of the invention comprises treating an organoboron compound, which organoboron compound comprises a boron atom bonded to an sp.sup.2 hybridized carbon atom, with (i) .sup.18F and (ii) a copper compound. The invention also provides the use of an organoboron compound, which organoboron compound comprises a boron atom bonded to an sp.sup.2 hybridized carbon atom, in a process for producing an organic compound comprising an .sup.18F atom, which process comprises treating the organoboron compound with (i).sup.18F and (ii) a copper compound. The invention also provides a compound of formula (XXXVII): wherein: each PG.sup.A is independently H or an alcohol protecting group; PG.sup.B is H or a carboxylic acid protecting group; each PG.sup.C is independently an amine protecting group; Z is a group selected from a boronic ester group, a boronic acid group, a borate group, and a trifluoroborate group; and a is an integer from 0 to 4. ##STR00001##

AN IMPROVED ONE POT, ONE STEP PROCESS FOR THE HALOGENATION OF AROMATICS USING SOLID ACID CATALYSTS

The present invention disclosed an improved one pot, one step process for halogenation of compound of formula (II) to afford corresponding halogenated compound of formula (I) having improved yield and increased selectivity under very mild conditions.

AN IMPROVED ONE POT, ONE STEP PROCESS FOR THE HALOGENATION OF AROMATICS USING SOLID ACID CATALYSTS

The present invention disclosed an improved one pot, one step process for halogenation of compound of formula (II) to afford corresponding halogenated compound of formula (I) having improved yield and increased selectivity under very mild conditions.

AN IMPROVED ONE POT, ONE STEP PROCESS FOR THE HALOGENATION OF AROMATICS USING SOLID ACID CATALYSTS

The present invention disclosed an improved one pot, one step process for halogenation of compound of formula (II) to afford corresponding halogenated compound of formula (I) having improved yield and increased selectivity under very mild conditions.

BENZO-RING-CONTAINING DERIVATIVE, AND PREPARATION METHOD THEREFOR AND USE THEREOF

The present invention relates to a benzo-ring-containing derivative, and a preparation method therefor and the use thereof. Specifically, the present invention relates to a compound as represented by general formula (Ia), and a preparation method therefor, a pharmaceutical composition containing same, and the use thereof as a GABA receptor agonist in the field of the central nervous system, specifically in inducing and maintaining anesthesia of mammals.

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BENZO-RING-CONTAINING DERIVATIVE, AND PREPARATION METHOD THEREFOR AND USE THEREOF

The present invention relates to a benzo-ring-containing derivative, and a preparation method therefor and the use thereof. Specifically, the present invention relates to a compound as represented by general formula (Ia), and a preparation method therefor, a pharmaceutical composition containing same, and the use thereof as a GABA receptor agonist in the field of the central nervous system, specifically in inducing and maintaining anesthesia of mammals.

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Synthesis of phenylethynylbenzenes

A method of: reacting a dihydroxybenzene with bromine to form a bromodihydroxybenzene; reacting the bromodihydroxybenzene with trifluoromethanesulfonyl chloride or trifluoromethanesulfonic anhydride to form a bromotrifluoromethanesulfonatobenzene; and reacting the bromotrifluoromethanesulfonatobenzene with phenylacetylene to form a phenylethynylbenzene.

Synthesis of phenylethynylbenzenes

A method of: reacting a dihydroxybenzene with bromine to form a bromodihydroxybenzene; reacting the bromodihydroxybenzene with trifluoromethanesulfonyl chloride or trifluoromethanesulfonic anhydride to form a bromotrifluoromethanesulfonatobenzene; and reacting the bromotrifluoromethanesulfonatobenzene with phenylacetylene to form a phenylethynylbenzene.

Synthesis of phenylethynylbenzenes

A method of: reacting a dihydroxybenzene with bromine to form a bromodihydroxybenzene; reacting the bromodihydroxybenzene with trifluoromethanesulfonyl chloride or trifluoromethanesulfonic anhydride to form a bromotrifluoromethanesulfonatobenzene; and reacting the bromotrifluoromethanesulfonatobenzene with phenylacetylene to form a phenylethynylbenzene.

METATHESIS CATALYSTS AND METHODS THEREOF

The present application provides, among other things, compounds and methods for metathesis reactions. In some embodiments, the present disclosure provides methods for preparing alkenyl halide with regioselectivity and/or stereoselectivity. In some embodiments, the present disclosure provides methods for preparing alkenyl halide with regioselectivity and Z-selectivity. In some embodiments, the present disclosure provides methods for preparing alkenyl halide with regioselectivity and E-selectivity. In some embodiments, provided technologies are particularly useful for preparing alkenyl fluorides. In some embodiments, a provided compound useful for metathesis reactions has the structure of formula II-a. In some embodiments, a provided compound useful for metathesis reactions has the structure of formula II-b.