Patent classifications
C07B39/00
Method for preparing partially fluorinated alcohol
A method for preparing a partially fluorinated alcohol, comprises reacting an epoxide: wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are independently selected from the group comprising H, F, Cl, Br, I, CF.sub.3, alkyl, fluoroalkyl, haloalkyl with a fluorinating agent.
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.
Method and production line for preparing 2,6-dichloropyridine through gas phase photochlorination of pyridine
The present invention relates to a method for preparing 2,6-dichloropyridine with product purity greater than or equal to 99.0% through gas phase photochlorination of pyridine by using trifluoromethyl chlorobenzene as a solvent for reaction between pyridine and chlorine gas. Gasified pyridine and heated chlorine gas are enabled to continuously experience chlorination reaction under irradiation of ultraviolet light by using gasified pyridine and heated chlorine gas as starting materials and using heated trifluoromethyl chlorobenzene as a solvent, and a gas phase reaction product and the solvent are cooled to obtain pyridine chlorination solution. Advantages: firstly, it pioneers the precedent of direct and high-selectivity preparation of 2,6-dichloropyridine through gas phase photochlorination, and not only can the 2,6-dichloropyridine product with purity greater than or equal to 99.0% be obtained, but also industrial production is facilitated; and secondly, the selectivity of pyridine chlorination is high, the chlorination solution is subjected to crude distillation to separate high-boiling-point substances, the crude distillate is subjected to cooling crystallization or rectification to separate the solvent, the solvent is reused, and not only can the 2,6-dichloropyridine product with purity greater than or equal to 99.0% be obtained, but also the purposes of no pollution, low energy consumption and low cost can be realized.
Method and production line for preparing 2,6-dichloropyridine through gas phase photochlorination of pyridine
The present invention relates to a method for preparing 2,6-dichloropyridine with product purity greater than or equal to 99.0% through gas phase photochlorination of pyridine by using trifluoromethyl chlorobenzene as a solvent for reaction between pyridine and chlorine gas. Gasified pyridine and heated chlorine gas are enabled to continuously experience chlorination reaction under irradiation of ultraviolet light by using gasified pyridine and heated chlorine gas as starting materials and using heated trifluoromethyl chlorobenzene as a solvent, and a gas phase reaction product and the solvent are cooled to obtain pyridine chlorination solution. Advantages: firstly, it pioneers the precedent of direct and high-selectivity preparation of 2,6-dichloropyridine through gas phase photochlorination, and not only can the 2,6-dichloropyridine product with purity greater than or equal to 99.0% be obtained, but also industrial production is facilitated; and secondly, the selectivity of pyridine chlorination is high, the chlorination solution is subjected to crude distillation to separate high-boiling-point substances, the crude distillate is subjected to cooling crystallization or rectification to separate the solvent, the solvent is reused, and not only can the 2,6-dichloropyridine product with purity greater than or equal to 99.0% be obtained, but also the purposes of no pollution, low energy consumption and low cost can be realized.
METHOD FOR AROMATIC FLUORINATION
Disclosed is a f fluorination method comprising providing a fluorinating reagent and a solvent to a reaction mixture; providing a compound having the formula ArX to the reaction mixture; wherein, A is a aryl, substituted aryl, heteroaryl or substituted heteroaryl, and X is CI, Br, I or NO.sub.2, providing tetramethylammonium 2,6-dimethylphenolate to the reaction mixture; and reacting under conditions sufficient to provide a species having the formula ArF.
METHOD FOR AROMATIC FLUORINATION
Disclosed is a f fluorination method comprising providing a fluorinating reagent and a solvent to a reaction mixture; providing a compound having the formula ArX to the reaction mixture; wherein, A is a aryl, substituted aryl, heteroaryl or substituted heteroaryl, and X is CI, Br, I or NO.sub.2, providing tetramethylammonium 2,6-dimethylphenolate to the reaction mixture; and reacting under conditions sufficient to provide a species having the formula ArF.
Method of preparing benzyl 4-amino-3-chloro-5-fluoro-6-(4-chloro-2-fluoro-3-methoxyphenyl)picolinate
A method of preparing benzyl 4-amino-3-chloro-5-fluoro-6-(4-chloro-2-fluoro-3-methoxyphenyl)picolinate (I) from benzyl 4,5-difluoro-6-(4-chloro-2-fluoro-3-methoxyphenyl)picolinate (II) is described. The method includes the use of amination and chlorination process steps to provide the compound of Formula I.
Method of preparing benzyl 4-amino-3-chloro-5-fluoro-6-(4-chloro-2-fluoro-3-methoxyphenyl)picolinate
A method of preparing benzyl 4-amino-3-chloro-5-fluoro-6-(4-chloro-2-fluoro-3-methoxyphenyl)picolinate (I) from benzyl 4,5-difluoro-6-(4-chloro-2-fluoro-3-methoxyphenyl)picolinate (II) is described. The method includes the use of amination and chlorination process steps to provide the compound of Formula I.
Process for the preparation of organic bromides
The present invention provides a process for the preparation of organic bromides, by a radical bromodecarboxylation of carboxylic acids with a bromoisocyanurate.