Patent classifications
C07C315/04
COMPOUND AND PREPARATION METHOD AND APPLICATION THEREOF
The present disclosure relates to a compound and a preparation method and application thereof, the compound having a chemical structure formula of:
##STR00001##
wherein M in the formula is selected from a group consisting of CF.sub.3 or CF.sub.2H, and R.sub.1, R.sub.2, and R.sub.3 are each independently selected from a group consisting of aryl, heteroaryl, and alkyl. The compound provided by the present disclosure can be used as a trifluoroethanolation reagent or difluoroethanolation reagent as synthetic intermediates of many organic compounds, and some of the compounds have pharmaceutical activity. The preparation steps of such compounds are simplified, with mild synthesis conditions and wide applicability of substrates.
COMPOUND AND PREPARATION METHOD AND APPLICATION THEREOF
The present disclosure relates to a compound and a preparation method and application thereof, the compound having a chemical structure formula of:
##STR00001##
wherein M in the formula is selected from a group consisting of CF.sub.3 or CF.sub.2H, and R.sub.1, R.sub.2, and R.sub.3 are each independently selected from a group consisting of aryl, heteroaryl, and alkyl. The compound provided by the present disclosure can be used as a trifluoroethanolation reagent or difluoroethanolation reagent as synthetic intermediates of many organic compounds, and some of the compounds have pharmaceutical activity. The preparation steps of such compounds are simplified, with mild synthesis conditions and wide applicability of substrates.
PROCESS FOR MAKING HEPATITIS B CORE PROTEIN MODULATORS
The present disclosure provides, in part, a process for preparing compounds (I) having allosteric effector properties against Hepatitis B virus Cp.
##STR00001##
PROCESS FOR MAKING HEPATITIS B CORE PROTEIN MODULATORS
The present disclosure provides, in part, a process for preparing compounds (I) having allosteric effector properties against Hepatitis B virus Cp.
##STR00001##
PROCESSES FOR THE PREPARATION OF ORTHO-ALLYLATED HYDROXY ARYL COMPOUNDS
The present application describes process for preparing an ortho-allylated hydroxy aryl compounds such as compounds of Formula (I) by reacting an allylic alcohol with a hydroxy aryl compound in the presence of aluminum compound selected from alumina and aluminum alkoxides and in a non-protic solvent wherein at least one carbon atom ortho to the hydroxy group in the hydroxy aryl compound is unsubstituted. The present application also includes compounds of Formula (I).
##STR00001##
PROCESSES FOR THE PREPARATION OF ORTHO-ALLYLATED HYDROXY ARYL COMPOUNDS
The present application describes process for preparing an ortho-allylated hydroxy aryl compounds such as compounds of Formula (I) by reacting an allylic alcohol with a hydroxy aryl compound in the presence of aluminum compound selected from alumina and aluminum alkoxides and in a non-protic solvent wherein at least one carbon atom ortho to the hydroxy group in the hydroxy aryl compound is unsubstituted. The present application also includes compounds of Formula (I).
##STR00001##
Synthetic process
- William P. Gallagher ,
- John Ryan Coombs ,
- Carlos A. Guerrero ,
- David Marcoux ,
- Qing Shi ,
- Candice Lee Joe ,
- Sanjeewa Rupasinghe ,
- Jason J. Zhu ,
- Srinivas Kalidindi ,
- Sathasivam Shunmugaraj ,
- Moorthy Kandasamy ,
- Siva Sankar Bondigela ,
- Rajappa Vaidyanathan ,
- Shankar Tulsidas Tendulkar ,
- Sankar Kuppusamy ,
- Francisco González-Bobes
The invention generally relates to a process for preparing compounds, including Compound of Formula (I), useful as key intermediates in the preparation of compounds having RORγt antagonist properties. ##STR00001##
Synthetic process
- William P. Gallagher ,
- John Ryan Coombs ,
- Carlos A. Guerrero ,
- David Marcoux ,
- Qing Shi ,
- Candice Lee Joe ,
- Sanjeewa Rupasinghe ,
- Jason J. Zhu ,
- Srinivas Kalidindi ,
- Sathasivam Shunmugaraj ,
- Moorthy Kandasamy ,
- Siva Sankar Bondigela ,
- Rajappa Vaidyanathan ,
- Shankar Tulsidas Tendulkar ,
- Sankar Kuppusamy ,
- Francisco González-Bobes
The invention generally relates to a process for preparing compounds, including Compound of Formula (I), useful as key intermediates in the preparation of compounds having RORγt antagonist properties. ##STR00001##
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.