80360-14-1Relevant academic research and scientific papers
Mono-selective β-C-H arylation of: N -methylated amino acids and peptides promoted by the 2-(methylthio)aniline directing group
Kinsinger, Thorsten,Kazmaier, Uli
supporting information, p. 5595 - 5600 (2019/06/13)
2-(Methylthio)aniline (MTA) directed C(sp3)-H functionalisations are efficient and straightforward protocols for the selective β-modification of N-methylated amino acids. The decreased reactivity of MTA in comparison with the 8-aminoquinoline (AQ) directing group allows for selective monoarylations in high yields without the formation of side products. The protocol is also suitable for the introduction of highly functionalised side chains onto the C-terminal alanines of dipeptides. The MTA directing group can easily be removed, providing free carboxylic acids as valuable building blocks.
SELECTIVE INHIBITORS OF CLINICALLY IMPORTANT MUTANTS OF THE EGFR TYROSINE KINASE
-
Page/Page column 309, (2017/08/01)
The present invention provides compounds of Formula (I) or a subgeneric structure or species thereof, or a pharmaceutically acceptable salt, ester, solvate, and/or prodrug thereof, and methods and compositions for treating or ameliorating abnormal cell proliferative disorders, such as cancer, wherein A, R2, R3, R10, E1, E2, E3, Y, and Z are as defined herein.
Practical and efficient ipso-iodination of arylboronic acids via KF/I2 system
Tramutola, Francesco,Chiummiento, Lucia,Funicello, Maria,Lupattelli, Paolo
, p. 1122 - 1123 (2015/02/19)
A facile and effective iododeboronation of variously substituted aryl and heteroarylboronic acids through activation and subsequent ipso-introduction of iodine is presented. The use of KF and I2 at 80 °C in 1,4-dioxane furnishes iodinated compounds in high yields.
Convenient synthesis of bis(3-indolyl)-acetylene via Sonogashira coupling
Roy, Sudipta,Gribble, Gordon W.
, p. 829 - 837 (2008/02/01)
We describe the synthesis of bis(3-indolyl)acetylene 6 via a Pd-catalyzed cross-coupling reaction of iodoindole 8 and 3-indolylacetylene 9, followed by deprotection of 14 to furnish 6. Copyright Taylor & Francis Group, LLC.
Synthesis of indole analogs of 1-benzyl-3-(5'-hydroxymethy 1-2' -furyl) indazole (YC-1) as anti-platelet agents
-
Page/Page column 3, (2010/11/30)
The present invention synthesizes a series of novel indole analogs of 1-benzyl-3-(5′-hydroxymethyl-2′-furyl)indazole (YC-1), and their anti-platelet activity.
A simple iodination protocol via in situ generated ICl using NaI/FeCl 3
Mohanakrishnan, Arasambattu K.,Prakash, Chandran,Ramesh, Neelamegam
, p. 3242 - 3247 (2007/10/03)
A novel iodination of silyl-enol ethers using hitherto unexplored NaI/FeCl3 system is reported. The procedure has been extended to the iodination of aromatic and hetero aromatic compounds.
Facile and inexpensive entry to indeno[2,1-b]indol-6-one nucleus
Abbiati, Giorgio,Canevari, Valentina,Rossi, Elisabetta,Ruggeri, Alberto
, p. 1845 - 1850 (2007/10/03)
Starting from simple indole, a straightforward and inexpensive four-step synthetic approach to indeno[2,1-b]indol-6-one nucleus is described. Copyright Taylor & Francis, Inc.
Development of highly stereoselective asymmetric 6π- azaelectrocyclization of conformationally flexible linear 1-azatrienes. From determination of multifunctional chiral amines, 7-alkyl cis-1-amino-2-indanols, to application as a new synthetic strategy: Formal synthesis of 20-epiuleine
Tanaka, Katsunori,Kobayashi, Toyoharu,Mori, Hajime,Katsumura, Shigeo
, p. 5906 - 5925 (2007/10/03)
The highly stereoselective asymmetric 6π-azaelectrocyclization was achieved as a general synthetic method based on the reaction between the (E)-3-carbonyl-2,4,6-trienal compounds and the (-)-7-alkyl-cis-l-amino-2-indanol derivatives which are effective chiral amines. The 7-alkyl-substituted 2-indanol moiety of the cyclized products was efficiently removed by the novel manganese dioxide oxidation under remarkably mild conditions, and the method was successfully applied to the formal synthesis of optically active 20-epiuleine.
Rapid route to 3,4-substituted indoles via a directed ortho metalation-retro-Mannich sequence.
Chauder, Brian,Larkin, Andrew,Snieckus, Victor
, p. 815 - 817 (2007/10/03)
[reaction: see text] In the presence of NXS (X = Br, I, Cl), gramine derivatives 1, derived by combined directed ortho metalation (DoM)-cross-coupling sequences, rapidly undergo retro-Mannich fragmentation (2) to afford 3-halo indoles 3 in 37-88% yields.
Bis-Suzuki reactions of 2,3-dihaloindoles. A convenient synthesis of 2,3-diarylindoles
Liu,Gribble
, p. 8717 - 8721 (2007/10/03)
A convenient, one-pot synthesis of 2,3-diarylindoles 4 is described via a bis-Suzuki palladium-catalyzed cross coupling of 2,3-dihalo-1-(phenylsulfonyl)indoles 1 with arylboronic acids 2, followed by cleavage of the N-protecting group to give 4. The anti-inflammatory drug indoxole (4c) is prepared in high yield. (C) 2000 Elsevier Science Ltd.
