1296223-82-9Relevant articles and documents
KIF18A INHIBITORS
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Paragraph 0360; 0361, (2021/02/12)
Amide compounds of formula (I): and compositions containing them, and processes for preparing such compounds. Provided herein also are methods of treating disorders or diseases treatable by inhibition of Kinesin Motor Protein KIF18A, such as cancer, psoriasis, atopic dermatitis, an autoimmune disorder, or inflammatory bowel disease, and the like.
A chemoselective Reformatsky-Negishi approach to α-haloaryl esters
Wong, Brian,Linghu, Xin,Crawford, James J.,Drobnick, Joy,Lee, Wendy,Zhang, Haiming
, p. 1508 - 1515 (2014/02/14)
A practical synthesis of α-haloaryl esters has been achieved via a chemoselective Negishi coupling of poly-halogenated aromatics and Reformatsky reagents in the presence of catalytic Pd(dba)2 and Xantphos. This chemistry tolerates a variety of aryl halides and was successfully applied to the synthesis of Ibuprofen. The α-haloaryl ester products, exemplified by ethyl 2-(4-bromo-2-chlorophenyl)acetate (3a), can be further functionalized via palladium or copper catalysis to afford an array of α-aryl esters.
Cyclopropanation of substituted phenylacetonitriles or phenyl acetates
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Paragraph 0024, (2015/01/18)
The present invention relates to a process for the cyclopropanation with ethylene carbonate or ethylene sulfate of a compound of formula (II): wherein G is -CN or -COOR in which R is a C1-C4 straight or branched alkyl X and Y are independently selected from the group consisting of hydrogen, fluorine, chlorine, bromine, iodine, R1O- and R1S- wherein R1 is C1-C4 straight or branched alkyl chain.
PROCESS FOR THE PREPARATION OF DERIVATIVES OF 1-(2-FLUORO[1,1'-BIPHENYL]-4-YL)-CYCLOPROPANECARBOXYLIC ACID
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Paragraph 0061, (2015/01/07)
The present invention relates to a process for the preparation of a compound of formula (I) or a pharmaceutically acceptable salt thereof: wherein R represents one or more groups independently selected from fluorine, chlorine, bromine, and iodine, said process comprising the cyclopropanation of a compound of formula (II) with ethylene carbonate or ethylene sulfate: wherein X is chlorine, bromine, iodine or a triflate group (CF3SO3) or a group ?wherein R is as defined above and G is —CN or —COOR2 wherein R2 is a C1-C4 straight or branched alkyl chain.
IMPROVED PROCESS FOR THE PREPARATION OF DERIVATIVES OF 1-(2-FLUORO[1,1'-BIPHENYL]-4-YL)-CYCLOPROPANECARBOXYLIC ACID
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Page/Page column 9, (2015/01/16)
The present invention relates to a process for the preparation of a compound of formula (I) or a pharmaceutically acceptable salt thereof: formula (I) wherein R represents one or more groups independently selected from fluorine, chlorine, bromine, and iodine, said process comprising the cyclopropanation of a compound of formula (II) with ethylene carbonate or ethylene sulfate: formula (II) wherein X is chlorine, bromine, iodine or a triflate group (CF3SO3) or a group (formula) wherein R is as defined above and G is -CN or -COOR2 wherein R2 is a C1-C4 straight or branched alkyl chain.
