C07B39/00

Catalytic radiofluorination

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.

Methods for preparing bridged bi-aromatic ligands

New methods for preparing bridged bi-aromatic ligands are disclosed. The methods employ aryl coupling of unprotected phenols. The ligands may be used to prepare transition metal compounds useful as catalysts in olefin polymerization.

Methods for preparing bridged bi-aromatic ligands

New methods for preparing bridged bi-aromatic ligands are disclosed. The methods employ aryl coupling of unprotected phenols. The ligands may be used to prepare transition metal compounds useful as catalysts in olefin polymerization.

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.

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.

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.

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.

Structure and synthesis of highly fluorinated amino acid derivatives

Methods of synthesizing polyfluorinated amino acid derivatives are disclosed, along with polyfluorinated amino acid derivatives produced from said methods, as well as compositions containing same. The synthesis methods utilize an oxazolone and a perfluoroarene to produce the polyfluorinated amino acid derivatives.

PROCESSES FOR PREPARING AN FGFR INHIBITOR
20200148680 · 2020-05-14 ·

Disclosed herein are processes for preparing 8-(3-(4-acryloylpiperazin-1-yl)propyl)-6-(2,6-dichloro-3,5-dimethoxyphenyl)-2-(methylamino)pyrido[2,3-d]pyrimidin-7(8H)-one and FGFR inhibitor, as well as polymorphs and/or salt forms thereof.

PROCESSES FOR PREPARING AN FGFR INHIBITOR
20200148680 · 2020-05-14 ·

Disclosed herein are processes for preparing 8-(3-(4-acryloylpiperazin-1-yl)propyl)-6-(2,6-dichloro-3,5-dimethoxyphenyl)-2-(methylamino)pyrido[2,3-d]pyrimidin-7(8H)-one and FGFR inhibitor, as well as polymorphs and/or salt forms thereof.