C07B47/00

RADIOLABELING AGENTS, METHODS OF MAKING, AND METHODS OF USE THEREOF

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.

PHOSPHINE REAGENTS FOR AZINE FLUOROALKYLATION

A new set of bench-stable fluoroalkylphosphines that directly convert CH 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 CC bond formation.

PHOSPHINE REAGENTS FOR AZINE FLUOROALKYLATION

A new set of bench-stable fluoroalkylphosphines that directly convert CH 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 CC bond formation.

PROCESS FOR THE PREPARATION OF CRISABOROLE IN A STABLE CRYSTAL FORM

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##

METHOD OF 4-BORONOPHENYLALANINE PRODUCTION
20200392163 · 2020-12-17 ·

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.

Carbon dioxide as a directing group for C—H functionalization reactions involving Lewis basic amines, alcohols, thiols, and phosphines for the synthesis of compounds

Methods of synthesizing compounds using CO.sub.2 as a directing group for CH functionalization, and compounds made thereby, are described.

Carbon dioxide as a directing group for C—H functionalization reactions involving Lewis basic amines, alcohols, thiols, and phosphines for the synthesis of compounds

Methods of synthesizing compounds using CO.sub.2 as a directing group for CH functionalization, and compounds made thereby, are described.

Process for preparing platinum organosiloxane complexes

A platinum organosiloxane complex is prepared by a process including 1) combining A) a platinous halide and B) a ketone, and thereafter 2) adding C) a polyorganosiloxane having, per molecule, 2 to 4 silicon bonded terminally unsaturated hydrocarbon groups having from 2 to 6 carbon. The platinum organosiloxane complex prepared by the process is useful as a hydrosilylation catalyst.

Process for preparing platinum organosiloxane complexes using an enone additive

A platinum organosiloxane complex is prepared by a process including combining A) a platinous halide; B) a ketone; C) an enone additive distinct from any other starting materials or rearrangement products thereof; and D) a polyorganosiloxane having, per molecule, 2 to 4 silicon bonded terminally unsaturated hydrocarbon groups having from 2 to 6 carbon. The platinum organosiloxane complex prepared by the process is useful as a hydrosilylation catalyst.

Electro-polarizable compound and capacitor

An electro-polarizable compound has the following general formula: ##STR00001## where Core1 is an aromatic polycyclic conjugated molecule having two-dimensional flat form and self-assembling by pi-pi stacking in a column-like supramolecule, which is tetrapirolic macro-cyclic fragment, R1 is an dopant group connected to Core1, m is number of R1 which is equal to 1, 2, 3 or 4, R2 is a substituent comprising one or more ionic groups, p is number of R2 which is equal to 0, 1, 2, 3 or 4. The fragment marked NLE containing the Core1 with at least one R1 has a nonlinear effect of polarization. Core2 is an electro-conductive oligomer self-assembling by pi-pi stacking in a column-like supramolecule, n is number of Core2 which is equal to 2, or 4, R3 is a substituent comprising one or more ionic groups, s is number of R3 which is equal to 0, 1, 2, 3 or 4. R4 is a non-polar resistive substituent, k is a number of R4 which is equal to 0, 1, 2, 3, 4, 5, 6, 7 or 8.