28566-12-3Relevant academic research and scientific papers
A four-component domino reaction: An eco-compatible and highly efficient construction of 1,8-naphthyridine derivatives, their in silico molecular docking, drug likeness, ADME, and toxicity studies
Garg, Ankita,Tadesse, Aschalew,Eswaramoorthy, Rajalakshmanan
, (2021/04/26)
A multicomponent domino reaction of enaminone, malononitrile, and o-phthalaldehyde has been established, providing direct access to novel highly functionalized pentacyclic cyclopenta [b] indeno [1, 2, 3-de] [1,8] naphthyridine derivatives. The simplicity of execution, readily available substrates, high yields, excellent functional group tolerance, scalability, and good scores of environmental parameters make this synthetic strategy more sustainable and worthy of further attention. This one-pot transformation, which involved multiple steps and did not require the use of a catalyst, constructed four new C-C bonds, two new C-N bonds, and three new rings, with efficient use of all reactants. Furthermore, we performed in silico molecular docking analysis for prediction of anticancer (against human topoisomerase IIβ protein) and antimicrobial (against E.coli. DNA gyrase B protein) activities. Drug likeness and ADMET studies were also predicted. Overall investigation indicates that compound 6i may serve as a candidate that could be developed as potential anticancer and antimicrobial agent among all.
METHYL(R)-2-(FLUOROMETHYL)-5-OXO-4-PHENYL-4,5,6, 7-TETRAHYDRO-1H-CYCLOPENTA[B]PYRIDINE-3-CARBOXYLATE AND METHYL(R)-2-(FLUOROMETHYL)-5-OXO-4-PHENYL-1,4,5,7-TETRAHYDROFURO[3,4-B]PYRIDINE-3-CARBOXYLATE USED AS ACTIVATORS OF CAV1.2
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, (2022/01/05)
The invention relates to a compound according to formula (I) or a pharmaceutically acceptable salt thereof used as activators of CaV1.2 for the treatment of schizophrenia, bipolar disorder, major depressive disorder, ADHD, Phelan-McDermid syndrome, autism spectrum disorder, multiple sclerosis, frontotemporal dementia, Alzheimer's disease, Brugada syndrome, short QT syndrome or early repolarization syndrome.
Copper-Catalyzed Thiolation of Terminal Alkynes Employing Thiocyanate as the Sulfur Source Leading to Enaminone-Based Alkynyl Sulfides under Ambient Conditions
Chandran,Pise, Ashwini,Shah, Suraj Kumar,Rahul,Suman,Tiwari, Keshri Nath
supporting information, p. 6557 - 6561 (2020/08/24)
A highly efficient protocol for copper-catalyzed thio-alkynylation of enaminone-based thiocyanates with terminal alkynes under mild conditions has been developed. This scalable amino group-directed thio-alkynylation proceeds in the open air with a broad substrate scope and an excellent yield. The demonstrated synthetic transformation creates the opportunity for a wide variety of sulfur-containing useful materials. Gram-scale synthesis and further synthetic transformations of alkynyl sulfides highlight the potential utility of the method.
An expeditious access of 2,5′-dioxo-5′,6′,7′,8′-tetrahydro-1′H-spiro[indoline-3,4′-quinoline]-3′-carboxylate by reaction of isatin, ethyl cyanoacetate and enaminone in water
Tiwari, Keshri Nath,Prabhakaran,Kumar, Vaneet,Rajendra, Thakar Snehal,Mathew, Shintu
, p. 3596 - 3601 (2018/05/26)
We have demonstrated three component reaction of isatin, enaminone and ethyl cyanoacetate leading to sprirooxindole scaffold without catalyst in water. The synthetic protocol has several advantages like wide substrate scope, atom-economy and operationally simple experimental procedures which provides rapid access to library of compounds. The mechanistic details of the reaction has been investigated during the course of study.
Cu catalyzed cross-dehydrogenative coupling reaction for the synthesis of 3-hydroxy-2-pyrrolidinones
Sarkar, Rajib,Mukhopadhyay, Chhanda
, p. 3069 - 3076 (2018/07/06)
A new convenient strategy for the synthesis of 3-hydroxy-2-pyrrolidinone derivatives featuring regioselective C–C coupling has been developed. This is a Cu (II) catalyzed cross dehydrogenative coupling (CDC) involving enamino-ketones of benzyl amines and di-alkyl acetylenedicarboxylate, followed by cyclization by primary amines. TBHP (tert-butyl hydroperoxide) has been used as the oxidant to promote the coupling protocol. This synthetic route principally demonstrates the scope of CDC reaction and also applicable to gram-scale synthesis.
SUBSTITUTED OXOPYRIDINE DERIVATIVES AND USE THEREOF AS FACTOR XIA/PLASMA
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Paragraph 0328-0330, (2016/06/28)
The invention relates to substituted oxopyridine derivatives and to processes for their preparation, and also to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular cardiovascular disorders, preferably thrombotic or thromboembolic disorders, and oedemas, and also ophthalmic disorders.
Substituted oxopyridine derivatives and use thereof as factor XIA/plasma
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Paragraph 0196; 0197, (2016/10/09)
The invention relates to substituted oxopyridine derivatives of formula (I), in which n stands for the number 1 or 2, A stands for -N(R2)- or -CH2-, R1 stands for a group of formula (II), R3 and R4 stand for hydrogen, and R5 stands for a group of formula (III) or (IV), methods for producing said substituted oxopyridine derivatives, and use of said substituted oxopyridine derivatives to produce drugs for treating and/or preventing diseases, in particular cardiovascular diseases, preferably thrombotic or thromboembolic diseases, and edemas and ophthalmologic diseases.
An efficient synthesis of 3-aminocyclopent-2-en-1-one
Kikani,McKee,Zanger
, p. 176 - 176 (2007/10/02)
A two step, efficient synthesis of the key intermediate 3-aminocyclopent-2-en-1-one starting from 1,3-cyclopentanedione is described. This involves the reaction of ammonia gas with 3-ethoxycyclopent-2-en-1-one.
