150760-45-5Relevant academic research and scientific papers
Development of a manufacturing process for 1-(1-pyridin-2-yl methyl-piperidin-4-yl)-1H-indole: A key intermediate for protein kinase C inhibitor LY317615
Boini, Sathish,Moder, Kenneth P.,Vaid, Radhe K.,Kopach, Micheal,Kobierski
, p. 1205 - 1211 (2006)
This contribution describes process development leading to the production of 1-(1-pyridin-2-yl methyl-piperidin-4-yl)-1H-indole (11). The title compound 11 was produced via a Leimgruber-Batcho indole synthesis using key intermediates 2-(2,2-dimethoxyethyl
Application of the Cleavable Isocyanide in Efficient Approach to Pyroglutamic Acid Analogues with Potential Biological Activity
Jassem,Al-Ajely,Almashal,Chen
, p. 2562 - 2570 (2019)
Two efficient procedures have been developed for the synthesis of pyroglutamic acid analogues 28, 29, and 34. According to the first method the Ugi (4C3C) reaction is followed by a post-transformation reaction, and the second method involves the Michael a
TFA-catalysed tandem double cyclisation: A one-pot, metal-free routes for novel indolo-imidazo[1,2-a]pyridine derivatives
Ganesher, Asha,Panda, Gautam
, (2019)
A transition-metal free, one-pot tandem synthetic routes for novel indole and imidazo[1,2-a]pyridine derivative hybrids have been established. An efficient three-component reaction was designed with incorporation of two sequential Groebke–Blackburn–Bienay
COMPOUNDS USEFUL IN HIV THERAPY
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Page/Page column 139, (2020/06/19)
The invention relates to compounds of Formula (I), (Ia), (Ib), (II) or (III), salts thereof, pharmaceutical compositions thereof, as well as therapeutic methods of treatment and prevention.
New entry to convertible isocyanides for the Ugi reaction and its application to the stereocontrolled formal total synthesis of the proteasome inhibitor omuralide
Gilley, Cynthia B.,Buller, Matthew J.,Kobayashi, Yoshihisa
, p. 3631 - 3634 (2008/02/12)
The development of a new convertible isocyanide, indole-isocyanide, for ready access to pyroglutamic acids culminated in the formal total synthesis of the proteasome inhibitor omuralide featuring a stereocontrolled Ugi reaction. Indole-isocyanide was name
Strategies for the synthesis of N-(azacycloalkyl)bisindolylmaleimides: Selective inhibitors of PKCβ
Faul, Margaret M.,Grutsch, John L.,Kobierski, Michael E.,Kopach, Michael E.,Krumrich, Christine A.,Staszak, Michael A.,Udodong, Uko,Vicenzi, Jeffrey T.,Sullivan, Kevin A.
, p. 7215 - 7229 (2007/10/03)
N-(Azacycloalkyl)bisindolylmaleimides 1 have been identified to be selective inhibitors of PKCβ. This manuscript will describe the synthetic approaches employed to prepare this class of compounds that resulted in development of efficient methods for prepa
Synthesis of 3-methoxyquinolines via cyclization of 1-isocyano-2-(2-lithio-2-methoxyethenyl)benzenes
Kobayashi, Kazuhiro,Yoneda, Keiichi,Mizumoto, Tatsuya,Umakoshi, Hironobu,Morikawa, Osamu,Konishi, Hisatoshi
, p. 4733 - 4736 (2007/10/03)
2-(2-Isocyanophenyl)acetaldehyde dimethyl acetals were treated with excess LDA to generate 1-isocyano-2-(2-lithio-2-methoxyethenyl)benzenes, which cyclized intramolecularly to afford 3-methoxyquinolines in good to excellent yields.
2-(2-aminophenyl)-acetaldehyde dimethyl acetal: A novel reagent for the protection of carboxylic acids
Arai, Eri,Tokuyama, Hidetoshi,Linsell, Martin S.,Fukuyama, Tohru
, p. 71 - 74 (2007/10/03)
The synthesis and use of 2-(2-aminophenyl)-acetaldehyde dimethyl acetal 1 are described. The amides 2, derived from this amine and carboxylic acids, are stable under basic conditions and thus can be regarded as the protected carboxylic acids. The corresponding carboxylic acids are regenerated by conversion of 2 into indolylamides 3 by treatment with CSA and subsequent hydrolysis with LiOOH or NaOH. In addition, 3 can be easily converted to esters, amides, and aldehydes.
