70-23-5Relevant articles and documents
Method for synthesizing pharmaceutical intermediate 2-aminothiazole-4-ethyl formate
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Paragraph 0010, (2018/07/30)
The invention discloses a method for synthesizing a pharmaceutical intermediate 2-aminothiazole-4-ethyl formate, ethyl pyruvate, dichloromethane, concentrated sulfuric acid, bromine, ethyl bromopyruvate, thiourea and ethanol are used as main raw materials, and a main factor affecting the product yield during cyclization reaction is the ratio of the important intermediate ethyl bromopyruvate to thethiourea. According to experimental procedures, the ethanol is selected as a solvent, nanocatalyst Cu2O@HKUST-1 is added, under reflux conditions, a desired product with a higher yield can be obtained by optimizing of the material ratio, the intermediate catalyst used in the method shortens the reaction cycle, a solid carbonate is used to adjust the pH of the reaction liquid, the generation of wastewater is reduced, and economic benefits are increased.
A method for synthesizing pyrroloquinoline quinone (by machine translation)
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Paragraph 0029; 0040-0042, (2018/08/28)
The invention relates to a synthetic pyrroloquinoline quinone of the method, the method to pyruvic acid ethyl ester as the starting synthetic raw material, preparation pyrroloquinoline quinone. In the synthetic method of the present invention, compound 4 synthesis of compound 5 is the key step in the synthetic route, in the key step 5) in, the invention creative use of hexafluoro antimonate ion liquid, hexafluoro titanate ion liquid, six fluorine niobium acid salt ion liquid such as Lewis acid ionic liquid, the ionic liquid has the function of the reaction medium and the catalyst, thereby improving the response speed and the yield of this step. In addition, the invention preferably use the [BMIm] SbF6 Ionic liquid, [BMIm] SbF6 Ionic liquid and Sc (OTf)3 Can be formed of a higher catalytic activity [Sc (OTf)3 -x ] [SbF6 ], Can make the reaction efficiency is greatly improved, and the obtained reaction product in [BMIm] SbF6 The solubility of the ionic liquid in small, easily precipitated, so as to improve the reaction yield (can be up to 96%). (by machine translation)
A pharmaceutical intermediates for synthesis and its preparation method (by machine translation)
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Paragraph 0041; 0042, (2017/11/04)
The present invention discloses a pharmaceutical intermediates for synthesis and its preparation method, its structural formula is as follows: Wherein R1 C is hydrogen or1 - C4 The alkane, R2 For C1 - C4 The alkane. The intermediate for the synthesis of 2 - isopropyl-thiazole - 4 - carboxylic acid ethyl ester, every one-step reaction conditions are easy to control, product yield and purity are very high, the operating procedure is simplified, basic does not need to be purified, and further reducing the cost of the final product. (by machine translation)
Solvent-free synthesis of bacillamide analogues as novel cytotoxic and anti-inflammatory agents
Kumar, Sunil,Aggarwal, Ranjana,Kumar, Virender,Sadana, Rachna,Patel, Bhumi,Kaushik, Pawan,Kaushik, Dhirender
, p. 718 - 726 (2016/08/15)
Synthesis of fourteen analogues of bacillamide, a bioactive tryptamide alkaloid of marine origin, has been accomplished through a highly efficient convergent route. The present solvent-free protocol involves the formation of thiazole ring in the initial step followed by amide coupling between substituted ethyl 2-alkyl/aryl/heteroaryl/amino/aminoarylthiazole-4-carboxylates and tryptamine in presence of 2-hydroxy-4,6-dimethylpyrimidine, a solid phase catalyst to yield N-[2-(1H-indol-3-yl)ethyl]-2-alkyl/aryl/heteroaryl/amino/aminoarylthiazole-4-carboxamides as bacillamide analogues having structural variation at position-2 of thiazole ring. Bacillamide and its analogues were evaluated for their cytotoxic activity against three cancer cell lines (HCT-116, MDA-MD-231 and JURKAT cell lines) using colorimetric cell proliferation assay. Compounds 17a and 17b exhibited potent anti-cell proliferation activity with IC50values in the range of ～3.0?μM and ～0.1–0.6?μM, respectively against these cell lines. Preliminary mechanism of action studies indicates that these compounds initiate caspase dependent apoptosis. Also, compounds 16d, 16f, 17a and 17d exhibited excellent anti-inflammatory activity comparable to well-known NSAID indomethacin and better to bacillamide, when evaluated using carrageenan induced rat hind paw oedema method.
An efficient total synthesis of (-)-epothilone B
Wang, Jie,Sun, Bing-Feng,Cui, Kai,Lin, Guo-Qiang
supporting information, p. 6354 - 6357 (2013/02/23)
An efficient total synthesis of (-)-epothilone B has been achieved in ca. 8% yield over 11 steps from 9 (or 10 steps from 7/8), which features a bissiloxane-tethered ring closing metathesis reaction to approach the trisubstituted (Z) double bond and forms a new basis for further development of an industrial process for epothilone B and ixabepilone.
Discovery of imidazo[1,2-a]pyridines as potent MCH1R antagonists
Kishino, Hiroyuki,Moriya, Minoru,Sakuraba, Shunji,Sakamoto, Toshihiro,Takahashi, Hidekazu,Suzuki, Takao,Moriya, Ryuichi,Ito, Masahiko,Iwaasa, Hisashi,Takenaga, Norihiro,Ishihara, Akane,Kanatani, Akio,Sato, Nagaaki,Fukami, Takehiro
scheme or table, p. 4589 - 4593 (2010/04/25)
A series of imidazo[1,2-a]pyridine derivatives was identified and evaluated for MCH1R binding and antagonistic activity. Introduction of a methyl substituent at the 3-position of imidazo[1,2-a]pyridine provided compounds with a significant improvement in MCH1R affinity. Representative compounds in this series exhibited good potency and brain exposure in rats.
PROPYL 3-BROMO-2-OXOPROPIONATE AND DERIVATIVES AS NOVEL ANTICANCER AGENTS
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Page/Page column 59-60, (2008/06/13)
The present invention is directed to compositions that inhibit glycolysis, preferentially in cancer. Specifically, the anticancer compositions comprise 3-halo-2-oxopropionate and its derivatives, such as ester derivatives. However, in specific embodiments, the anticancer composition is sodium 3-halo-2-oxopropionate, such as sodium 3-bromo-2--oxopropionate and a stabilizing agent, such as carbonic acid. In particular embodiments, the compositions of the present invention further comprise a metabolic intermediate for normal cells to utilize in a pathway for an alternate energy source, thereby providing protection to normal cells. In other embodiments, the 3-halo-2-oxopropionate or its ester derivative is used in combination with an additional cancer therapy, such as radiation and/or a drug.
Scavenger assisted combinatorial process for preparing libraries of tertiary amine compounds
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, (2008/06/13)
This invention relates to a novel solution phase process for the preparation of tertiary amine combinatorial libraries. These libraries have utility for drug discovery and are used to form wellplate components of novel assay kits.
Synthesis and antibacterial activity of some imidazo[1,2-a[pyrimidine derivatives
Rival,Grassy,Michel
, p. 1170 - 1176 (2007/10/02)
A series of 75 imidazo[1,2-a]pyrimidine derivatives were synthesized. The 'in vitro' antibacterial activity of these compounds and their corresponding α-bromoketones against a variety of gram (+), gram (-) bacteria and Mycobacterium species is reported. Some of the prepared derivatives exhibited potent antimicrobial activity.
N-THIAZOLYLMETHYLTHIOALKYL-N`-ALKENYL (OR ALKYNYL)GUANIDINES AND RELATED COMPOUNDS
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, (2008/06/13)
N-alkenyl (or N-alkynyl)-N'-2-(aminoalkyl)-4-thiazolylmethylthio!alkylguanidines, thioureas, ethenediamines and related compounds, H 2 receptor antagonists, useful in inhibiting gastric acid secretion in mammals.
