Patent classifications
C07D213/61
Method for aromatic fluorination
Disclosed is a fluorination method comprising providing an aryl fluorosulfonate and a fluorinating reagent to a reaction mixture; and reacting the aryl fluorosulfonate and the fluorinating reagent to provide a fluorinated aryl species. Also disclosed is a fluorination method comprising providing, a salt comprising a cation and an aryloxylate, and SO.sub.2F.sub.2 to a reaction mixture; reacting the SO.sub.2F.sub.2 and the ammonium salt to provide a fluorinated aryl species. Further disclosed a fluorination method comprising providing a compound having the structure Ar—OH to a reaction mixture; where Ar is an aryl or heteroaryl; providing SO.sub.2F.sub.2 to the reaction mixture; providing a fluorinating reagent to the reaction mixture; reacting the SO.sub.2F.sub.2, the fluorinating reagent and the compound having the structure Ar—OH to provide a fluorinated aryl species having the structure Ar—F.
Compounds for inhibition of α4β7 integrin
- Peter A. Blomgren ,
- Taryn Campbell ,
- Jayaraman Chandrasekhar ,
- Christopher T. Clark ,
- Julian A. Codelli ,
- Kevin S. Currie ,
- Jeffrey E. Kropf ,
- Yasamin Moazami ,
- Nicole Nava ,
- Leena Patel ,
- Stephane Perreault ,
- Jason K. Perry ,
- Kassandra F. Sedillo ,
- Natalie Seeger ,
- Kirk L. Stevens ,
- Jennifer Anne Treiberg ,
- Suet C. Yeung ,
- Zhongdong Zhao
The present disclosure provides a compound of Formula (I): ##STR00001##
or a pharmaceutically acceptable salt thereof as described herein. The present disclosure also provides pharmaceutical compositions comprising a compound of Formula (I), processes for preparing compounds of Formula (I), and therapeutic methods for treating inflammatory disease.
NITRATION
A process for preparing a nitrated compound, including the step of reacting a compound (A) including at least one substituted or unsubstituted aromatic or heteroaromatic ring, wherein the heteroaromatic ring includes at least one heteroatom selected from the group consisting of oxygen, sulfur, phosphor, selenium and nitrogen, with a compound of formula (I)
##STR00001##
wherein Y is selected from the group consisting of hydrogen and nitro.
METHODS AND INTERMEDIATES FOR PREPARING THERAPEUTIC COMPOUNDS
- Kevin McCormack Allan ,
- Amanda Lynn Vandehey ,
- Gediminas Brizgys ,
- Sachin Dhar ,
- Ian James Doxsee ,
- Alex Goldberg ,
- Lars V. Heumann ,
- Zilin Huang ,
- Nathaniel Thomas Kadunce ,
- Shahrokh Kazerani ,
- Willard Lew ,
- Vinh Xuan Ngo ,
- Brian Michael O'Keefe ,
- Trevor James Rainey ,
- Benjamin James Roberts ,
- Bing Shi ,
- Dietrich P. Steinhuebel ,
- Winston C. Tse ,
- Anna Michelle Wagner ,
- Xianghong Wang ,
- Scott Alan Wolckenhauer ,
- Chloe Yuyi Wong ,
- Jennifer R. Zhang
The present disclosure relates to methods and intermediates useful for preparing a compound of formula I.
##STR00001##
or a co-crystal, solvate, salt or combination thereof.
METHODS AND INTERMEDIATES FOR PREPARING THERAPEUTIC COMPOUNDS
- Kevin McCormack Allan ,
- Amanda Lynn Vandehey ,
- Gediminas Brizgys ,
- Sachin Dhar ,
- Ian James Doxsee ,
- Alex Goldberg ,
- Lars V. Heumann ,
- Zilin Huang ,
- Nathaniel Thomas Kadunce ,
- Shahrokh Kazerani ,
- Willard Lew ,
- Vinh Xuan Ngo ,
- Brian Michael O'Keefe ,
- Trevor James Rainey ,
- Benjamin James Roberts ,
- Bing Shi ,
- Dietrich P. Steinhuebel ,
- Winston C. Tse ,
- Anna Michelle Wagner ,
- Xianghong Wang ,
- Scott Alan Wolckenhauer ,
- Chloe Yuyi Wong ,
- Jennifer R. Zhang
The present disclosure relates to methods and intermediates useful for preparing a compound of formula I.
##STR00001##
or a co-crystal, solvate, salt or combination thereof.
HETEROCYCLIC COMPOUND
A compound represented by formula (I)
##STR00001## or an N-oxide compound thereof is provided with excellent control efficacies against harmful arthropods, wherein A.sup.1 represents a nitrogen atom or a CR.sup.4; R.sup.4 represents a hydrogen atom, a OR.sup.27, a NR.sup.27R.sup.28, a cyano group, a nitro group, or a halogen atom;
##STR00002##
hereinafter referred to as “Het”, represents Het-1, Het-2, Het-3, or Het-4:
##STR00003## wherein #.sup.1 represents the binding position of Het and T, and #.sup.2 represents the binding position of Het and
##STR00004## T represents T-1, T-2, T-3, T-4, T-5, T-6, or T-7:
##STR00005## R.sup.1 represents a C1-C10 chain hydrocarbon group having one or more halogen atoms or the like; and R.sup.2 represents a C1-C6 alkyl group optionally having one or more halogen atoms or the like.
HETEROCYCLIC COMPOUND
A compound represented by formula (I)
##STR00001## or an N-oxide compound thereof is provided with excellent control efficacies against harmful arthropods, wherein A.sup.1 represents a nitrogen atom or a CR.sup.4; R.sup.4 represents a hydrogen atom, a OR.sup.27, a NR.sup.27R.sup.28, a cyano group, a nitro group, or a halogen atom;
##STR00002##
hereinafter referred to as “Het”, represents Het-1, Het-2, Het-3, or Het-4:
##STR00003## wherein #.sup.1 represents the binding position of Het and T, and #.sup.2 represents the binding position of Het and
##STR00004## T represents T-1, T-2, T-3, T-4, T-5, T-6, or T-7:
##STR00005## R.sup.1 represents a C1-C10 chain hydrocarbon group having one or more halogen atoms or the like; and R.sup.2 represents a C1-C6 alkyl group optionally having one or more halogen atoms or the like.
PROCESS OF MANUFACTURE OF A COMPOUND FOR INHIBITING THE ACTIVITY OF SHP2, AS WELL AS PRODUCTS RESULTING FROM ACID ADDITION
The invention relates to a method for the manufacture of a compound of Formula I as mentioned above, or a pharmaceutically acceptable salt, acid co-crystal, hydrate or other solvate thereof, said method comprising reacting a compound of the formula II with a compound of the formula III according to the following reaction scheme: wherein A, LG, n and m are as defined in the Summary of the Invention.
##STR00001##
METHOD FOR PREPARING 2,3-DICHLORO-5-TRIFLUOROMETHYLPYRIDINE WITH HIGH SELECTIVITY
A method for preparing 2,3-dichloro-5-trifluoromethylpyridine, comprising at a temperature of 100˜150° C. and a pressure of 0.5˜5.0 MP, in presence of at least one catalyst selected from supported metal chloride, supported zeolite molecular sieve and supported heteropolyacid, 2-chloro-5-trifluoromethylpyridine reacts with chlorine gas to obtain 2,3-dichloro-5-trifluoromethylpyridine. The preparing method provided by the present invention has advantages such as high selectivity of desired product, high utilization rate of chlorine gas, moderate process condition, simple operation and less three wastes. The present invention also discloses a preparing method for preparing 2-chloro-5-trifluoromethylpyridine, which is capable of reducing unit consumption, reducing separation cost, and improving safety compared to the prior art.
METHOD FOR PREPARING 2,3-DICHLORO-5-TRIFLUOROMETHYLPYRIDINE WITH HIGH SELECTIVITY
A method for preparing 2,3-dichloro-5-trifluoromethylpyridine, comprising at a temperature of 100˜150° C. and a pressure of 0.5˜5.0 MP, in presence of at least one catalyst selected from supported metal chloride, supported zeolite molecular sieve and supported heteropolyacid, 2-chloro-5-trifluoromethylpyridine reacts with chlorine gas to obtain 2,3-dichloro-5-trifluoromethylpyridine. The preparing method provided by the present invention has advantages such as high selectivity of desired product, high utilization rate of chlorine gas, moderate process condition, simple operation and less three wastes. The present invention also discloses a preparing method for preparing 2-chloro-5-trifluoromethylpyridine, which is capable of reducing unit consumption, reducing separation cost, and improving safety compared to the prior art.