A new set of bench-stable fluoroalkylphosphines that directly convert C—H bonds in pyridine building blocks, drug-like fragments, and pharmaceuticals, into fluoroalkyl derivatives. No pre-installed functional groups or directing motifs are required. The reaction tolerates a variety of sterically and electronically distinct pyridines and is exclusively selective for the 4-position in most cases. The reaction proceeds via initial phosphonium salt formation followed by sp.sup.2-sp.sup.3 phosphorus ligand-coupling, an underdeveloped manifold for C—C bond formation.

The synthesis and structure of beta-diketiminate manganese compounds are described, as well as their use as catalysts for the hydrosilylation and hydroboration of unsaturated organic compounds and main group element-main group element bond formation via dehydrogenative coupling.

The synthesis and structure of beta-diketiminate manganese compounds are described, as well as their use as catalysts for the hydrosilylation and hydroboration of unsaturated organic compounds and main group element-main group element bond formation via dehydrogenative coupling.

The present invention relates to a method of production of 4-boronophenylalanine (BPA) from 4-iodophenylalanine, in which all the functional groups of the amino acid are protected by benzyl protection method, and which uses isopropyl magnesium halogenide stabilized by a complexation base, and subsequent condensation of the resulting Grignard reagent with a boric acid ester. The final reaction step, catalytic hydrogenolysis or transfer hydrogenolysis of protecting groups on the amino acid, occurs after hydrolysis of the boronate ester groups.

Methods for preparing active carbonate esters of water-soluble polymers are provided. Also provided are other methods related to the active carbonate esters of water-soluble polymers, as well as corresponding compositions.

Methods for preparing active carbonate esters of water-soluble polymers are provided. Also provided are other methods related to the active carbonate esters of water-soluble polymers, as well as corresponding compositions.

A catalytic process for the metal-free functionalization of sp.sup.2-carbons is described herein. The catalytic process is suitable for forming borylated alkenes, arenes and heteroarenes and comprises the use of catalysts comprising a Frustrated Lewis Pair (FLP).

A catalytic process for the metal-free functionalization of sp.sup.2-carbons is described herein. The catalytic process is suitable for forming borylated alkenes, arenes and heteroarenes and comprises the use of catalysts comprising a Frustrated Lewis Pair (FLP).

The present invention relates to a process for the preparation of crisaborole of formula (I):

##STR00001##

by preparing intermediates of formulas (II) and (III):

##STR00002##

Described herein are labeling agents, specifically [.sup.11C]fluoroform, [.sup.11C]difluoromethane, [.sup.11C]fluoromethyl iodide, [.sup.11C]fluoromethyl bromide, [.sup.11C]fluoromethyl chloride, [.sup.11C]fluoromethyl trifluoromethansulfonate, [.sup.11C]difluoromethyl iodide, [.sup.11C]difluoromethyl bromide, [.sup.11C]difluoromethyl chloride, [.sup.11C]difluoromethyl trifluoromethansulfonate, [.sup.11C]trifluoromethyl iodide, [.sup.11C]trifluoromethyl bromide, [.sup.11C]trifluoromethyl chloride, [.sup.11C]trifluoromethyl trifluoromethansulfonate, [.sup.18]fluoroform, [.sup.18F]difluoromethane, [.sup.18F]difluoromethyl bromide or [.sup.18F]trifluoromethyl bromide. Also included are methods of labeling precursors to provide labeled fluoroalkanes and imaging methods.