82294-70-0Relevant articles and documents
Synthesis method of 4-methylthiazole-5-formaldehyde
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Paragraph 0028; 0031; 0034-0036; 0039-0041; 0044-0045, (2021/05/01)
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.
Novel synthesis method of 4-methylthiazole-5-formaldehyde
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Paragraph 0022-0030, (2021/05/12)
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.
Dimethyl sulfoxide-accelerated reductive deamination of aromatic amines with t-BuONO in tetrahydrofuran
Fang, Lu,Qi, Liang,Ye, Longfei,Pan, Zhentao,Luo, Wenjun,Ling, Fei,Zhong, Weihui
, p. 579 - 583 (2018/11/27)
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.
Novel preparation method for 4-methylthiazole-5-carboxaldehyde
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Paragraph 0040; 0045; 0046; 0047; 0048; 0049; 0050, (2019/01/14)
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.
PYRAZOLE DERIVATIVES AS MODULATORS OF CALCIUM RELEASE -ACTIVATED CALCIUM CHANNEL
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Page/Page column 70-71, (2011/04/26)
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.
HETEROARYL COMPOUNDS AS PDE10A INHIBITORS
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Page/Page column 39, (2011/11/06)
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.
Concise synthesis of vinylheterocycles through β-elimination under solventless phase transfer catalysis conditions
Albanese, Domenico,Ghidoli, Cristina,Zenoni, Maurizio
, p. 736 - 739 (2013/01/03)
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.
Efficient and eco-friendly preparation of 4-methyl-5-formyl-thiazole
Bai, Nan,Sha, Yaowu,Meng, Ge
, p. 943 - 947 (2008/09/20)
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.
PREPARATION OF INTERMEDIATE FOR 3-[2-(4-METHYLTHIAZOLE-5-YL)VINYL] CEPHALOSPORINS
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Page/Page column 11, (2008/06/13)
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.
The oxidation of alcohols in N-oxyl-immobilized silica gel/aqueous NaOCl disperse systems. A prominent access to a column-flow system
Tanaka, Hideo,Chou, Jingyu,Mine, Machiko,Kuroboshi, Manabu
, p. 1745 - 1755 (2007/10/03)
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.