C07B39/00

C-HALOGEN BOND FORMATION

Methods of halogenating a carbon containing compound having an sp3 CH bond are provided. Methods of fluorinating a carbon containing compound comprising halogenation with Cl or Br followed by nucleophilic substitution with F are provided. Methods of direct oxidative CH fluorination of a carbon containing compound having an sp3 CH bond are provided. The halogenated products of the methods are provided.

Complexes for Nucleophilic, Radical, and Electrophilic Polyfluoroalkylation
20190127397 · 2019-05-02 ·

Disclosed herein are borazine complexes and use of the same in perfluoroalkylation reactions.

ARYL ETHERS AND USES THEREOF

The present disclosure relates to HIF-2? inhibitors and methods of making and using them for treating cancer. Certain compounds were potent in HIF-2? scintillation proximity assay, luciferase assay, and VEGF ELISA assay, and led to tumor size reduction and regression in 786-O xenograft bearing mice in vivo.

Method for producing dichloro addition product of aliphatic olefin by photocatalysis under visible light

The invention provides a method for producing a dichloro addition product of an aliphatic olefin by photocatalysis under visible light. The method includes reacting an aliphatic olefin as a substrate with hydrochloric acid as a chlorine source in an organic solvent under visible light irradiation in the presence of copper chloride with visible light absorption ability as a catalyst, to obtain the dichloro addition product of the aliphatic olefin, wherein the reaction is carried out under an oxygen-containing atmosphere, the aliphatic olefin comprises a carbon-carbon double bond and a C9-C15 aliphatic chain connected to the carbon-carbon double bond by a covalent bond. In the invention, visible light is used to provide the energy and a transition metal chloride with visible light absorption ability is used to undergo light-induced electron transfer from chloride with a reaction substrate, thereby initiating an addition reaction to obtain a dichloro addition product.

Method for producing dichloro addition product of aliphatic olefin by photocatalysis under visible light

The invention provides a method for producing a dichloro addition product of an aliphatic olefin by photocatalysis under visible light. The method includes reacting an aliphatic olefin as a substrate with hydrochloric acid as a chlorine source in an organic solvent under visible light irradiation in the presence of copper chloride with visible light absorption ability as a catalyst, to obtain the dichloro addition product of the aliphatic olefin, wherein the reaction is carried out under an oxygen-containing atmosphere, the aliphatic olefin comprises a carbon-carbon double bond and a C9-C15 aliphatic chain connected to the carbon-carbon double bond by a covalent bond. In the invention, visible light is used to provide the energy and a transition metal chloride with visible light absorption ability is used to undergo light-induced electron transfer from chloride with a reaction substrate, thereby initiating an addition reaction to obtain a dichloro addition product.

Chlorination of sucrose-6-esters

There is provided a method for the chlorination of a sucrose-6-acylate to produce a 4,1,6-trichloro-4,1,6-trideoxy-galactosucrose-6-acylate, wherein said method comprises the following steps (i) to (v): (i) providing a first component comprising sucrose-6-acylate; (ii) providing a second component comprising a chlorinating agent; (iii) combining said first component and said second component to afford a mixture; (iv) heating said mixture for a heating period in order to provide chlorination of sucrose-6-acylate at the 4, 1 and 6 positions thereof; (v) quenching said mixture to produce a 4,1,6-trichloro-4,1,6-trideoxy-galactosucrose-6-acylate; wherein at least one of said first component and said second component comprises a reaction vehicle, and said reaction vehicle comprises a tertiary amide; and wherein said mixture comprises a cosolvent during a least a portion of the heating period of step (iv), wherein said cosolvent comprises perfluorooctane.

Chlorination of sucrose-6-esters

There is provided a method for the chlorination of a sucrose-6-acylate to produce a 4,1,6-trichloro-4,1,6-trideoxy-galactosucrose-6-acylate, wherein said method comprises the following steps (i) to (v): (i) providing a first component comprising sucrose-6-acylate; (ii) providing a second component comprising a chlorinating agent; (iii) combining said first component and said second component to afford a mixture; (iv) heating said mixture for a heating period in order to provide chlorination of sucrose-6-acylate at the 4, 1 and 6 positions thereof; (v) quenching said mixture to produce a 4,1,6-trichloro-4,1,6-trideoxy-galactosucrose-6-acylate; wherein at least one of said first component and said second component comprises a reaction vehicle, and said reaction vehicle comprises a tertiary amide; and wherein said mixture comprises a cosolvent during a least a portion of the heating period of step (iv), wherein said cosolvent comprises perfluorooctane.

CATALYTIC RADIOFLUORINATION
20190054198 · 2019-02-21 ·

One aspect of the present invention relates to a method of preparing radiofluorinated substituted alkyl, cycloalkyl, aryl, and alkenyl compounds. In a preferred embodiment, potassium fluoride-18 is used. Another aspect of the invention relates to piperazine compounds containing fluorine-18 that are useful as imaging agents. In certain embodiments, the piperazine compounds contain a quaternary amine. Another aspect of the invention relates to arylphosphonium compounds containing fluorine-18 that are useful as imaging agents. In certain embodiments, the phosphonium compound is a tetraaryl phosphonium salt. Another aspect of the present invention relates to a method of obtaining a positron emission image of a mammal, comprising the steps of administering to a mammal a compound of the invention, and acquiring a positron emission spectrum of the mammal.

FEEDING PROCESS OF CHLORINE FLUORIDE

A chlorine fluoride feeding device and feeding process are provided that can stably generate industrially applicable chlorine fluoride (ClF), control flow rate, and provide continual feed.

The feeding process of chlorine fluoride of this invention is a feeding process to feed chlorine fluoride generated by loading a gas that contains fluorine atoms and a gas that contains chlorine atoms to a flow-type heat reactor or a plasma reactor, and it can stably generate and safely feed chlorine fluoride for a long time by reacting chlorine fluoride that is difficult to pack at a high pressure, such that an amount that can be packed in a gas container such as a gas cylinder is limited, with two or more types of gas materials that can be packed safely in a gas container by liquefaction, or with such gas material and a solid material.

ISOTOPIC FLUORINATION AND APPLICATIONS THEREOF
20180362432 · 2018-12-20 ·

Methods of CH bond fluorination using non-heme manganese catalyst are described herein. For example, a method comprises providing a reaction mixture including a non-heme manganese catalyst, a substrate comprising an sp.sup.3 CH bond and a fluorinating agent and converting the sp.sup.3 CH bond to a CF bond in the presence of the non-heme manganese catalyst or a derivative thereof.