22581-33-5Relevant academic research and scientific papers
Iron-catalyzed preparation of trifluoromethyl substituted vinyl- and alkynylcyclopropanes
Morandi, Bill,Cheang, Jeremy,Carreira, Erick M.
, p. 3080 - 3081 (2011)
A convenient iron-catalyzed procedure to prepare trifluoromethylated vinyl- and alkynylcyclopropanes in a chemo- and diastereoselective manner is presented. The active diazo compound (trifluoromethyl diazomethane) is generated in situ and used in the conc
Fluoroalkyl-substituted cyclopropane derivatives: Synthesis and physicochemical properties
Grygorenko, Oleksandr O.,Chernykh, Anton V.,Olifir, Oleksandr S.,Kuchkovska, Yuliya O.,Volochnyuk, Dmitriy M.,Yarmolchuk, Vladimir S.
, p. 12692 - 12702 (2020/11/10)
A series of all 12 cis- and trans-cyclopropanecarboxylic acids and cyclopropylamines bearing CH2F, CHF2, and CF3 substituents were synthesized by different methods on a multigram scale. Dissociation constants (pKa) and log P values were measured for the o
BICYCLIC JAK INHIBITORS AND USES THEREOF
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Paragraph 000351; 000353, (2020/10/20)
Provided herein are compounds of Formulas (I), (II), (III), and (IV) and subformulas thereof, wherein the variables are defined herein. Also provided herein are pharmaceutical compositions comprising a compound of Formula (I), (II), (III), or (IV) and methods of using the compounds, e.g., in the treatment of immune disorders, inflammatory disorders, and cancer.
PYRIDINE-1-OXIDE DERIVATIVES AND THEIR USE AS FACTOR XIA INHIBITORS
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Page/Page column 47, (2018/03/25)
The present invention provides a compound of Formula (I) and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing thromboses, embolisms, hypercoagulability or fibrotic changes. The compounds are selective Factor XIa inhibitors or dual inhibitors of Factor XIa and plasma kallikrein.
Piperazine derivatives and their use as therapeutic agents
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Paragraph 0115, (2016/03/19)
Compounds for treating an SCD-mediated disease or condition in a mammal, preferably a human, are disclosed, wherein the compounds are of formula (I): where x y, W, V, R 2 , R 3 , R 4 , R 5 , R 6 , R 6a , R 7 , R 7a , R 8 , R 8a , R 9 and R 9a are defined herein. Pharmaceutical compositions comprising the compounds of formula (I) are also disclosed.
(2R,1'S,2'R)- And (2S,1'S,2'R)-3-[2-mono(di,tri)fluoromethylcyclopropyl] alanines and their incorporation into hormaomycin analogues
De Meijere, Armin,Kozhushkov, Sergei I.,Yufit, Dmitrii S.,Grosse, Christian,Kaiser, Marcel,Raev, Vitaly A.
supporting information, p. 2844 - 2857 (2015/02/19)
Efficient and scalable syntheses of enantiomerically pure (2 R ,1' S ,2' R )- and (2 S ,1' S ,2' R )-3-[2-mono(di,tri)fluoromethylcyclopropyl] alanines 9a - c , as well as allo-D-threonine ( 4 ) and ( 2 S,3R)-β-methylphenylalanine (3), using the Belokon' approach with (S )- and (R )-2-[( N-benzylprolyl)amino]benzophenone [(S)- and (R)-10 ] as reusable chiral auxiliaries have been developed. Three new fluoromethyl analogues of the naturally occurring octadepsipeptide hormaomycin ( 1 ) with (fluoromethylcyclopropyl) alanine moieties have been synthesized and subjected to preliminary tests of their antibiotic activity.
An efficient and safe method for the multigram synthesis of trans -2-(trifluoromethyl)cyclopropylamine
Yarmolchuk, Vladimir S.,Bezdudny, Andrii V.,Tolmacheva, Nataliya A.,Lukin, Oleg,Boyko, Alexander N.,Chekotylo, Alexey,Tolmachev, Andrei A.,Mykhailiuk, Pavel K.
experimental part, p. 1152 - 1154 (2012/06/04)
trans-2-(Trifluoromethyl)cyclopropylamine was prepared on a multigram scale from readily accessible 4,4,4-trifluorobut-2-enoic acid in five steps. The key step was a high-yielding cyclopropane ring formation from 4,4,4-trifluorobut-2- enoic acid methoxymethyl amide under Corey-Chaykovsky reaction conditions. Georg Thieme Verlag Stuttgart New York.
Regioselectivity in the Ring Opening of 2-Alkylcyclopropylmethyl Radicals: the Effect of Electronegative Substituents
Ratier, Max,Pereyre, Michel,Davies, Alwyn G.,Sutcliffe, Roger
, p. 1907 - 1916 (2007/10/02)
The regioselectivity of the ring-opening of the trans-2-alkylcyclopropylmethyl radical A to give the primary alkyl radicals B, or the secondary alkyl radicals C, has been investigated, where the groups R and/or CXY carry electronegative substituents.All these reactions gave principally the secondary alkyl radicals C, whereas, in the absence of electronegative substituents, ring-opening occurs in favour of the primary alkyl radicals B.This regioselectivity is interpreted in terms of the frontier orbital interactions which are involved.
