5472-38-8Relevant academic research and scientific papers
Synthesis method of thiazolidinopyrimidinone acetic acid
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Paragraph 0024-0026; 0030-0032; 0035-0037, (2021/11/10)
The synthesis method comprises the following specific steps: (1) the compound II is a raw material, tetrahydrofuran is taken as a solvent, and the compound III is generated by reacting with ethyl formate under the action of sodium hydride. (2) Compound III and Compound V react in absolute ethanol to form compound IV. (3) Compound IV reacted with methanesulfonic acid in glacial acetic acid to form thiazolidinopyrimidinone acetic acid, i.e. compound i. The present invention is simple to operate, high in yield and suitable for industrial production.
CYCLIN-DEPENDENT KINASE INHIBITORS
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Page/Page column 268-269, (2020/07/15)
Described herein are compounds and their pharmaceutically acceptable salts, pharmaceutical compositions thereof, methods of treatment, and medical uses. The compounds described herein are modulators of cyclin-dependent kinases, and are useful in the treatment or alleviation of protein kinase associated disorders, including cancer, infectious diseases, autoimmune diseases, or cardiovascular diseases.
Insecticide dinotefuran intermediate 3 - hydroxy methyl tetrahydrofuran synthetic method
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Paragraph 0031; 0045; 0046; 0047, (2018/04/01)
The invention discloses a synthetic method of pesticide dinotefuran intermediate 3-hydroxymethyl tetrahydrofuran, and the synthetic method is as follows: reacting compound succinic acid dialkyl ester with formic acid alkyl ester in the presence of a strong alkali to obtain a compound III, then obtaining a compound II by a reduction reaction, finally, in the presence of an acid catalyst, obtaining a compound shown as formula I by a dehydration cyclization reaction, and R or R ' respectively independently represents C1-5 alkyl. The synthetic method is low in raw material cost, simple in reaction operation, less in pollution, high in yield of each step, 99% in the yield of the reducing step, and suitable for industrial production.
Synthesis and in?vitro evaluation of new fluorinated quinoline derivatives with high affinity for PDE5: Towards the development of new PET neuroimaging probes
Liu, Jianrong,Maisonial-Besset, Aurélie,Wenzel, Barbara,Canitrot, Damien,Baufond, Ariane,Chezal, Jean-Michel,Brust, Peter,Moreau, Emmanuel
, p. 548 - 560 (2017/05/24)
The increasing incidence of Alzheimer's disease (AD) worldwide is a major public health problem. Current treatments provide only palliative solutions with significant side effects. Therefore, new efficient treatment options and novel early diagnosis tools are urgently needed. Recently, strong pre-clinical evidences suggested that phosphodiesterase 5 (PDE5) may be clinically relevant both as biomarker and drug-target in AD. In this study, we intended to develop a new radiofluorinated tracer for the visualisation of PDE5 in brain using PET imaging. Based on currently known PDE5 inhibitors, a series of novel fluorinated compounds bearing a quinoline core have been synthesised via multi-steps reaction pathways. Their affinity for PDE5 and selectivity over other PDE families have been investigated. According to the data collected from this in vitro screening, fluorinated derivatives 24a, b bearing a fluoroethoxy group at the C-3 position of the quinoline core appeared to be the most promising structures and will be further radiolabelled with fluorine-18 for in vitro and in vivo evaluations as PET radiotracer for neuroimaging of PDE5.
Asymmetric Reduction of Lactam-Based β-Aminoacrylates. Synthesis of Heterocyclic β2-Amino Acids
Campello, Hugo Rego,Parker, Jeremy,Perry, Matthew,Ryberg, Per,Gallagher, Timothy
supporting information, p. 4124 - 4127 (2016/08/30)
The ability to affect asymmetric reduction of heterocyclic β-aminoacrylates 1 (n = 1-3) has been assessed with pyrrolidine and piperidone variants generating the corresponding N-heterocyclic β2-amino acids 3b and 5b with high enantioselectivity
HETEROCYCLIC CGRP RECEPTOR ANTAGONISTS
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Page/Page column 72, (2016/05/19)
The present invention is directed to heterocyclic compounds which are antagonists of CGRP receptors and may be useful in the treatment or prevention of diseases in which CGRP is involved, such as migraine. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.
FAK AND FLT3 INHIBITORS
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Page/Page column 132-133, (2014/03/22)
The use of a compound of the formula (I): (Formula (I)) in the preparation of a medicament for treating Acute Myeloid Leukemia or a disease ameliorated by the inhibition of Flt3, or Flt3 and FAK.
HETEROCYCLIC PYRIMIDINE CARBONIC ACID DERIVATIVES WHICH ARE USEFUL IN THE TREATMENT, AMELIORATION OR PREVENTION OF A VIRAL DISEASE
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Paragraph 0535-0537, (2013/12/04)
The present invention relates to a compound having the general formula (C), optionally in the form of a pharmaceutically acceptable salt, solvate, polymorph, codrug, cocrystal, prodrug, tautomer, racemate, enantiomer, or diastereomer or mixture thereof, which are useful in treating, ameliorating or preventing a viral disease. Furthermore, specific combination therapies are disclosed.
7-OXO-THIAZOLOPYRIDINE CARBONIC ACID DERIVATIVES AND THEIR USE IN THE TREATMENT, AMELIORATION OR PREVENTION OF A VIRAL DISEASE
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Paragraph 0536-0538, (2013/12/04)
The present invention relates to a compound having the general formula (A), optionally in the form of a pharmaceutically acceptable salt, solvate, polymorph, codrug, cocrystal, prodrug, tautomer, racemate, enantiomer, or diastereomer or mixture thereof, which are useful in treating, ameloriating or preventing a viral disease. Furthermore, specific combination therapies are disclosed.
FAK INHIBITORS
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Page/Page column 130; 131, (2012/09/10)
A compound of the formula (I): where R1 or R2 is a cycle amine group and R5 is an aromatic group with a carbonyl containing substituent for use as a FAK inhibitor.
