- Synthesis method of 4-methylthiazole-5-formaldehyde
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The invention provides a synthesis method of 4-methylthiazole-5-formaldehyde. The method comprises the following steps: 1) dissolving 4-methylthiazole-5-ethanol in a solvent, and carrying out oxidation reaction in the presence of a catalyst to obtain 4-methylthiazole-5-acetic acid; and 2) carrying out heating reaction on the 4-methylthiazole-5-acetic acid obtained in the step 1) in the presence of oxygen and a metal salt catalyst to obtain the 4-methylthiazole-5-formaldehyde. According to the method, 4-methylthiazole-5-ethanol is used as a raw material, the raw material is green, cheap and easy to obtain, the reaction process is mild in condition and environmentally friendly, the result selectivity is good, the yield is high, good economic benefits are achieved, and the method is suitable for industrial production.
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Paragraph 0028; 0031; 0034-0036; 0039-0041; 0044-0045
(2021/05/01)
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- Novel synthesis method of 4-methylthiazole-5-formaldehyde
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The invention provides a novel synthesis method of 4-methylthiazole-5-formaldehyde, which comprises the following steps: by taking 4-methylthiazole-5-methanol as a raw material, carrying out catalytic oxidation reaction to obtain the 4-methylthiazole-5-formaldehyde. In the catalytic oxidation reaction, an oxidant is molecular oxygen (oxygen or air), and a catalytic system is composed of a catalyst A, a catalyst B and a catalyst C. The catalyst A is piperidine nitroxide free radicals and derivatives thereof, the catalyst B is nitrogen oxides and equivalents thereof, and the catalyst C is protonic acid, bromides or ferric iron salt. The reaction raw materials are green and cheap, the catalytic system is efficient and environmentally friendly, the whole reaction process is clean and safe, and the method has great advantages from the perspective of economy or environmental protection.
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Paragraph 0022-0030
(2021/05/12)
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- Novel preparation method for 4-methylthiazole-5-carboxaldehyde
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The invention discloses a novel preparation method of 4-methylthiazole-5-carboxaldehyde. The novel preparation method includes the steps of subjecting 2-amino-4-methylthiazole to amino methylation toobtain 2-methylamino-4-methylthiazole, subjecting the 2-methylamino-4-methylthiazole to Vilsmeier reaction to obtain 2-methylamino-4-methyl-5-thiazolecarboxaldehyde, and hydrogenating the 2-methylamino-4-methyl-5-thiazolecarboxaldehyde to remove methylamino to obtain the 4-methylthiazole-5-carboxaldehyde. The preparation method has the advantages of moderate reaction condition, high yield, less generated waste and suitability for mass industrial production.
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Paragraph 0040; 0045; 0046; 0047; 0048; 0049; 0050
(2019/01/14)
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- Dimethyl sulfoxide-accelerated reductive deamination of aromatic amines with t-BuONO in tetrahydrofuran
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An efficient method for the conversion of aryl amines into arenes by a one-pot reductive deamination has been achieved. It was found the reductive deamination using t-BuONO in tetrahydrofuran could be accelerated by dimethyl sulfoxide and provided the deamination products with good yields under mild conditions. A plausible mechanism is discussed.
- Fang, Lu,Qi, Liang,Ye, Longfei,Pan, Zhentao,Luo, Wenjun,Ling, Fei,Zhong, Weihui
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p. 579 - 583
(2018/11/27)
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- PYRAZOLE DERIVATIVES AS MODULATORS OF CALCIUM RELEASE -ACTIVATED CALCIUM CHANNEL
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Disclosed are novel calcium release-activated calcium (CRAC) channel inhibitors, methods for preparing them, pharmaceutical compositions containing them, and methods of treatment using them. The present disclosure also relates to methods for treating non-small cell lung cancer (NSCLC) with CRAC inhibitors, and to methods for identifying therapeutics for treating and of diagnosing cancer.
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- HETEROARYL COMPOUNDS AS PDE10A INHIBITORS
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The present invention provides heteroaryl compounds as Phosphodiesterase 10A (PDE I OA) inhibitors. In particular, compounds described herein are useful for treating or preventing diseases, conditions and/or disorders by inhibiting Phosphodiesterase 10A enzyme. Also provided herein are processes for preparing compounds described herein, Formula (I), intermediates used in their synthesis, pharmaceutical compositions thereof.
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Page/Page column 39
(2011/11/06)
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- Concise synthesis of vinylheterocycles through β-elimination under solventless phase transfer catalysis conditions
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Various vinylheterocycles compounds have been prepared in excellent yields through β-elimination of the corresponding sulfonate esters with 50% aq NaOH under phase transfer catalysis conditions without organic solvent. The new approach provides an economic and environmentally friendly solution to removal of hazardous bases as well as toxic and expensive dipolar aprotic solvents.
- Albanese, Domenico,Ghidoli, Cristina,Zenoni, Maurizio
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p. 736 - 739
(2013/01/03)
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- Efficient and eco-friendly preparation of 4-methyl-5-formyl-thiazole
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4-Methyl-5-formylthiazole, an intermediate for synthesizing cefditoren pivoxil, was prepared in good yield by Pd/BaSO4 catalyzed hydrogenation of 4-methylthiazole-5-carboxylic acid chloride. Detailed reaction conditions have been studied.
- Bai, Nan,Sha, Yaowu,Meng, Ge
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p. 943 - 947
(2008/09/20)
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- PREPARATION OF INTERMEDIATE FOR 3-[2-(4-METHYLTHIAZOLE-5-YL)VINYL] CEPHALOSPORINS
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The present invention relates to the preparation of 4-methylthiazol-5-carboxaldehyde of Formula I, and use thereof as an intermediate in preparation of 3-[2-(4-methylthiazole-5-yl)vinyl] cephalosporins.
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Page/Page column 11
(2008/06/13)
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- The oxidation of alcohols in N-oxyl-immobilized silica gel/aqueous NaOCl disperse systems. A prominent access to a column-flow system
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The oxidation of alcohols was performed successfully in a disperse system with N-oxyl-adsorbed or immobilized silica gel as a disperse phase and aqueous NaOCl as a disperse medium. In the disperse system, the oxidation of sec-alcohols afforded the corresponding ketones, while prim-alcohols were oxidized to aldehydes and/or carboxylic acids depending on their structures and reaction conditions. The N-oxyl-immobilized silica gel was recovered and repeatedly used without a significant change in the product yields. A column-flow system was also investigated for the oxidation of alcohols by use of a newly devised column packed with the N-oxyl-immobilized silica gel.
- Tanaka, Hideo,Chou, Jingyu,Mine, Machiko,Kuroboshi, Manabu
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p. 1745 - 1755
(2007/10/03)
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- Process for the preparation of thiazole intermediate
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The present invention provides a process for the preparation of 4-methyl-5-formyl-thiazole of the formula (I) which comprises reducing the thiazole ester of the formula (III) to thiazole alcohol of the formula (IV), using sodium borohydride in the presence of AlCl3 in a solvent and oxidising using an oxidizing agent the thiazole alcohol of the formula (IV) to obtain 4-methyl-5-formyl-thiazole of the formula (I).
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Page/Page column 2
(2008/06/13)
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- A facile and selective synthetic method for the preparation of aromatic dialdehydes from diesters via the amine-modified SMEAH reduction system
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A new reduction system employing N-methylpiperazine-modified sodium bis(2-methoxyethoxy)aluminum hydride (NMP-SMEAH) for the conversion of aromatic diesters to dialdehydes is described. The method is plain and efficient, and can be carried out under mild and operationally simple conditions applicable for large scale productions.
- Hagiya, Kazutake,Mitsui, Sunao,Taguchi, Hiroaki
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p. 823 - 828
(2007/10/03)
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- BENZAZEPINE DERIVATIVES, PROCESS FOR THE PREPARATION OF THE SAME AND USES THEREOF
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Compounds of the general formula (I): or salts thereof, which exhibit CCR5 antagonism and exert preventive and therapeutic effects against HIV infections: wherein R1 is a 5- to 6-membered aromatic ring which bears a substituent represented by the general formula: R-Z1-X-Z2- (wherein R1 is hydrogen or optionally substituted hydrocarbyl; X is optionally substituted alkylene; and Z1 and Z2 are each a heteroatom) and may be further substituted, with R being optionally bonded to the aromatic ring to form another ring; Y is optionally substituted imino; and R2 and R3 are each optionally substituted aliphatic hydrocarbyl or an optionally substituted hetero-alicyclic group.
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- Inhibitors of protein isoprenyl transferases
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The present invention relates to novel compounds of Formula I which are useful in inhibiting protein isoprenyl transferases and the farnesylation or geranylgeranylation of the oncogene protein Ras and other related small g-proteins, and compositions containing such compounds and methods of using such compounds.
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- Cephalosporin derivatives and processes for the preparation thereof
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PCT No. PCT/KR96/00255 Sec. 371 Date Jun. 26, 1998 Sec. 102(e) Date Jun. 26, 1998 PCT Filed Dec. 27, 1996 PCT Pub. No. WO97/24359 PCT Pub. Date Jul. 10, 1997The invention provides novel cephalosporin derivatives of the formula (I) and salts thereof for use in pharmaceutical compositions. Also novel precursors for synthesis of the cephalosporins are disclosed.
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- Selective Bromination of 4,5-Dimethylthiazole with N-Bromosuccinimide
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Radical bromination of 4,5-dimethylthiazole (1) was carried out using different stoichiometries of N-bromosuccinimide in the presence of 2,2'-azobisisobutyronitrile.Mono-, tri- and tetrabromo compounds 2, 5, and 6 were obtained in good yields with regioselectivity while the dibromo derivatives 3 and 4 were formed without any selectivity.Substitution at the thiazole ring occurred in the presence of silica gel or in the perfluoro ether FC-77 (C8F16O), affording the 2-bromothiazole 7.The order of reactivity observed was 5-Me > 4-Me > C-2.Structural assignment of compounds 2-7 was made by chemical correlations and NMR spectroscopy. - Keywords: Heterocycles; NBS bromination; Selective bromination; Polybrominated thiazole; Structure elucidation
- Hariri, Mouaffak Al,Galley, Olivier,Pautet, Felix,Fillion, Houda
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p. 593 - 594
(2007/10/03)
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- Thiamin Biosynthesis in Yeast. Origin of the Five-Carbon Unit of the Thiazole Moiety
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Radioactivity from D--, D--, and D-glucose, from D-fructose, and from glycerol is incorporated nonrandomly into the C5 chain of the thiazole moiety of thiamin in Saccharomyces cerevisiae.The incorporation pattern leads to inference that the C5 chain is derived from a 2-pentulose, which is generated from the hexose precursors by the oxidative as well as by the nonoxidative pentose phosphate pathway.A chemically rational scheme for the biogenesis of the thiazole moiety of thiamin is presented.
- White, Robert L.,Spenser, Ian D.
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p. 4934 - 4943
(2007/10/02)
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