103858-53-3Relevant articles and documents
Synthesis method for preparing 2-substituted indole derivative
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Paragraph 0187-0190, (2019/05/28)
The invention relates to a synthesis method for preparing a 2-substituted indole derivative. The method includes the following steps: mixing aromatic amine compounds (I), ketone compounds (II) and a drying agent in an organic solvent; adding a palladium catalyst; and reacting in an aerobic weak acid environment to prepare the indole compounds (III). (I), (II) and (III) are as shown in the specification, wherein R1 is selected from hydrogen, C1-C6 alkyl, C1-C6 alkoxy, C1-C6 alkanoyl, C2-C6 alkenyl, C2-C6 alkynyl, halogen, hydroxyl, substituted or unsubstituted amino, substituted or unsubstituted phenyl, pyridyl and heterocyclic aryl; (I) can be pyridylamine, pyrimidylamine, pyridazinam or pyrazinamide which may further be substituted or unsubstituted; and the substituents are selected fromone or more C1-C6 alkyl, C1-C6 alkoxy, C1-C6 alkanoyl, C2-C6 alkenyl, C2-C6 alkynyl, halogen, hydroxyl, amino; and R2 is selected from C1-C6 alkyl, formate groups or C1-C6 alkylamide groups.
Carboxylic Acid-Promoted Single-Step Indole Construction from Simple Anilines and Ketones via Aerobic Cross-Dehydrogenative Coupling
Ren, Long,Nan, Guanglei,Wang, Yongcheng,Xiao, Zhiyan
, p. 14472 - 14488 (2018/11/23)
The cross-dehydrogenative coupling (CDC) reaction is an efficient strategy for indole synthesis. However, most CDC methods require special substrates, and the presence of inherent groups limits the versatility for further transformation. A carboxylic acid-promoted aerobic catalytic system is developed herein for a single-step synthesis of indoles from simple anilines and ketones. This versatile system is featured by the broad substrate scope and the use of ambient oxygen as an oxidant and is convenient and economical for both laboratory and industry applications. The existence of the labile hydrogen at C-3 and the highly transformable carbonyl at C-2 makes the indoles versatile building blocks for organic synthesis in different contexts. Computational studies based on the density functional theory (DFT) suggest that the rate-determining step is carboxylic acid-assisted condensation of the substrates, rather than the functionalization of aryl C-H. Accordingly, a pathway via imine intermediates is deemed to be the preferred mechanism. In contrast to the general deduction, the in situ formed imine, instead of its enamine isomer, is believed to be involved in the first ligand exchange and later carbopalladation of the α-Me, which shed new light on this indolization mechanism.
INDOLE DERIVATIVES AS EFFLUX PUMP INHIBITORS
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Page/Page column 198-199, (2018/09/28)
Disclosed herein are compounds of formula (I): and salts thereof. Also disclosed are compositions comprising compounds of formula I and compounds of formula I for use in treating or preventing bacterial infections.
INDOLE DERIVATIVE, PREPARATION METHOD THEREOF, AND USE THEREOF IN PHARMACEUTICAL DRUG
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Paragraph 0133; 0134, (2018/07/06)
An indole derivative as expressed by Formula (I), a preparation method thereof, a pharmaceutical salt, and use thereof as a therapeutic agent, especially as a FGFR inhibitor. Each substituent in Formula (I) has identical definition as specified in the specification.
NOVEL COMPOUND, PROCESS FOR THE PREPARATION THEREOF AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME
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, (2017/09/26)
The present invention relates to a novel compound controlling the phosphorylation of PPARandgamma; by CDK5, a process for the preparation thereof, and a pharmaceutical composition comprising the same. The novel compound of the present invention combines t
ZrCl4-promoted facile synthesis of indole derivatives
Tummatorn,Gleeson,Krajangsri,Thongsornkleeb,Ruchirawat
, p. 20048 - 20052 (2014/05/20)
Zirconium(iv) chloride effectively activates nitrogen (N2) extrusion from aryl azidoacrylates followed by annulation to provide the desired indole products in moderate to good yields. The reaction proceeds at low temperature and in short reaction time and is applicable to a variety of substrates.
Efficient synthesis of 2-ethoxycarbonyl indoles
Sudhakara,Jayadevappa,Mahadevan,Hulikal, Vijaykumar
experimental part, p. 2506 - 2515 (2009/12/06)
An efficient one-pot procedure for the synthesis of 2-ethoxycarbonyl indoles from commercially available materials has been developed. The one-step procedure involves in situ formation of the hydrazones from phenylhydrazine hydrochloride and ethyl pyruvate in the presence of bismuth nitrate followed by Fischer cyclization in polyphosphoric acid and ethanol. This method is efficient and simple.
Palladium-Catalyzed Regioselective Hydrodebromination of Dibromoindoles: Application to the Enantioselective Synthesis of Indolodioxane U86192A
Chae, Junghyun,Buchwald, Stephen L.
, p. 3336 - 3339 (2007/10/03)
A novel approach to the selective preparation of 4-bromoindoles was developed via Pd(OAc)2/rac-BINAP catalytic reactions. A variety of 4,6-dibromoindoles were transformed to 4-bromoindoles with high regioselectivity. This methodology, along wit
Cyclic compounds and uses thereof
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, (2008/06/13)
Compounds of general formula (1) R1—X1—W—X2—Z1—Z2—R2 or salts thereof, exhibiting preventive and therapeutic effects against HIV infectious diseases wherein R1is an optionally substituted five- or six-membered ring group; X1is a free valency or the like; W is a divalent group represented by, e. g., general formula (2) (wherein A and B are each an optionally substituted five- to seven-membered ring; E1and E4are each optionally substituted carbon or the like; E2and E3are each oxygen or the like; and a and b are each a single bond or a double bond); X2is a divalent group constituting a straight chain moiety; Z1is a divalent cyclic group or the like; Z2is a free valency or the like; and R2is optionally substituted amino or the like.
The first potent and selective non-imidazole human histamine H4 receptor antagonists
Jablonowski, Jill A.,Grice, Cheryl A.,Chai, Wenying,Dvorak, Curt A.,Venable, Jennifer D.,Kwok, Annette K.,Ly, Kiev S.,Wei, Jianmei,Baker, Sherry M.,Desai, Pragnya J.,Jiang, Wen,Wilson, Sandy J.,Thurmond, Robin L.,Karlsson, Lars,Edwards, James P.,Lovenberg, Timothy W.,Carruthers, Nicholas I.
, p. 3957 - 3960 (2007/10/03)
Following the discovery of the human histamine H4 receptor, a high throughput screen of our corporate compound collection identified compound 6 as a potential lead. Investigation of the SAR resulted in the discovery of novel compounds 10e and 10l, which are the first potent and selective histamine H4 receptor antagonists to be described.
