72850-76-1Relevant academic research and scientific papers
Synthetic method of drug intermediate sulfur-containing nitrogen heterocyclic amine compound (by machine translation)
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, (2020/09/12)
To the invention, 4 -N-BOC -3 - isopropylthiazole is obtained by reaction of 2 - methyl -4 - oxo-pentanoic acid ethyl ester, dichloromethane and sulfonyl chloride as a raw material, and then -3 - N-BOC - 2 - isopropylthiazole and HCl are added in the presence of ethanol as a solvent to obtain -4 - N-BOC-n-isopropythiazol -5 - methyl 4 -isoprop -5 -aminothiazole in the presence of triethylamine, and a NaOH solution is added as a solvent and then subjected to extraction washing to obtain 4 -yl -5 -aminothiazolethyl acetate in the presence of trifluoroethanol as a solvent and ethanol as a solvent to obtain ethyl acetate 4 - 5-propyl thiazole -5 - formic acid ethyl ester with ethanol as a 4 - solvent and an aqueous solution of N-BOC-5 n-isopropylthiazole 4 - and the like 4 -5 . The method has the advantages of clear steps, less waste, high yield, raw material saving and easy operation. (by machine translation)
Synthesis and biological activity of ethyl 2-(5-methyl-3-arylisoxazole-4-carboxamido)-4-alkylthiazole-5-carboxylate
Wang, Wei,Wang, Lie-Ping,Mao, Min-Zhen,Zhang, Xiao-Guang,Zheng, Xiao-Rui,Huang, Xiao-Ying,Xue, Chao,Ning, Bin-Ke
, p. 164 - 167 (2017/11/20)
A series of novel ethyl 2-(5-methyl-3-arylisoxazole-4-carboxamido)-4-alkylthiazole-5-carboxylates I-1-6 were synthesized. The structures of all target compounds were characterized by 1H NMR, 13C NMR, IR,MS and elemental analyses. Their fungicidal and herbicidal activities were evaluated. The results of preliminary bioassays show that the title compounds I-4 possess 20-50% inhibition against most of the tested plants at the dosage of 150 g ai/ha, while the title compounds I-1-5 possess 32-58% inhibition against FusaHum graminearum, Thanatephorus cucumeris, Botrytis cinereapers and Fusarium oxysporum in vitro at the concentration of 100 mg/L.
SUBSTITUTED AMINO-ACRYLCARBOXAMIDES AS KCNQ2/3 MODULATORS
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, (2014/06/11)
The invention relates to amino-arylcarboxamides, to pharmaceutical compositions containing these compounds and also to these compounds for use in the treatment and/or prophylaxis of pain and further diseases and/or disorders.
SUBSTITUTED AMINO-ARYLCARBOXAMIDES AS KCNQ2/3 MODULATORS
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, (2014/06/23)
The invention relates to amino-arylcarboxamides of formula (I), to pharmaceutical compositions containing these compounds and also to these compounds for use In the treatment and/or prophylaxis of pain and further diseases and/or disorders.
Xanthan sulfuric acid: An efficient bio-supported and recyclable solid acid catalyst for the synthesis of 2-aminothiazole-5-carboxylates and 2-aminoselenazole-5-carboxylates
Kuarm, Bowroju S.,Madhav, Janganati V.,Rajitha, Bhargavi
experimental part, p. 549 - 553 (2012/06/04)
An efficient method has been developed for the synthesis of 2-amino thiazole and selenazole-5-carboxylates from β-ketoesters, thiourea or seleno urea and N-bromo succinamide by using Xanthan sulfuric acid as a solid acid catalyst. The reaction work-up is
IMIDAZOLE CARBONYL COMPOUND
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Page/Page column 48, (2010/09/17)
To develop an antibiotic having a novel mechanism of action, the present inventors have searched for a compound that has weak cytotoxicity, the physical property of high solubility in water, the effect of inhibiting both DNA gyrase GyrB and topoisomerase IV ParE subunits, and sufficient antibacterial activity. As a result, the present inventors have completed the present invention by finding that a compound of the present invention represented by the general formula (1), a pharmacologically acceptable salt thereof, and a prodrug thereof have desirable properties. The present invention provides a pharmaceutical composition (particularly, a preventive or therapeutic composition for infectious disease) comprising a compound represented by the formula (1), a pharmacologically acceptable salt thereof, or a prodrug thereof as an active ingredient.
SUBSTITUTED PIPERIDINES AS CCR3 ANTAGONISTS
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Page/Page column 47, (2010/11/03)
Object of the present invention are novel substituted compounds of the formula 1, wherein A, R1, R2, R3 and R4 are defined as in the description. Another object of the present invention is to provide antagonists of CCR3, more particularly to provide pharmaceutical compositions comprising a pharmaceutically acceptable carrier and a therapeutically effective amount of at least one of the compounds of the present invention or a pharmaceutically acceptable salt thereof.
METHYL SULFANYL PYRMIDMES USEFUL AS ANTIINFLAMMATORIES, ANALGESICS, AND ANTIEPILEPTICS
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Page/Page column 159, (2010/12/18)
The present invention relates to pyrimidine derivatives of Formula (Ia) and (Ib) (including tautomers, isomers, prodrugs, and pharmaceutically acceptable salts thereof). Said compounds are useful in the treatment of pain (such as neuropathic pain), inflammation, and epilepsy (by acting as anticonvulsants). Methods of medical treatment making use of said compounds, as well as additional compounds of Formula (IIa) and (IIb), are also disclosed.
COMPOUNDS AND METHODS FOR MODULATING FXR
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Page/Page column 18, (2008/06/13)
Compounds of formula. wherein variables are as defined herein and their pharmaceutical compositions and methods of use are disclosed as useful for treating dyslipidemia and related diseases.
Aqueous-phase one-pot synthesis of 2-aminothiazole- or 2-aminoselenazole-5- carboxylates from β-keto esters, thiourea or selenourea, and N-bromosuccinimide under supramolecular catalysis
Narender, Mendu,Reddy, Majjigapu Somi,Kumar, Vydyula Pavan,Srinivas, Boga,Sridhar, Regati,Nageswar, Yadavalli Venkata Durga,Rao, Kakulapati Rama
, p. 3469 - 3472 (2008/09/19)
2-Amino-4-alkyl- and 2-amino-4-arylthiazole-5-carboxylates and their selenazole analogues were synthesized by α-halogenation of β-keto esters with N-bromosuccinimide, followed by cyclization with thiourea or selenourea, respectively, in the presence of β-
