cas 161798-02-3, Ethyl 2-(3-Cyano-4-hydroxyphenyl)-4-methyl-1,3-thiazole-5-carboxylate

Articles about 161798-02-3Total 9 be found

A practical oxidative conversion of aldehydes into N-chloroaldimines
A novel method for the preparation of N-chloroaldimines from commonly available aromatic aldehydes has been developed. The reaction proceeded effectively by two steps: aldehydes were initially transformed into imines and then chloro-substitution with NaClO2 gave the N-chloroaldimines. This simple protocol allows for the preparation of a variety of aromatic N-chloroaldimines in moderate to excellent yields without the isolation of the imine intermediate. We also found that 3-nitrobenzaldehyde and 4-cyanobenzaldehyde were converted into the related benzonitrile directly under the standard conditions.
Jin, Can,Wang, Feng,Sun, Bin,Zhuang, Xiaohui
p. 547 - 551
(2018/11/27)

Method for preparing Febuxostat through one-pot process
The invention provides a method for preparing Febuxostat through a one-pot process. The method comprises the following steps: (1) preparing a compound III from a compound II, after a reaction is completed, carrying out direct concentrating and drying, and directly carrying out a subsequent reaction without treatment; (2) under the condition of the presence of an acid binding agent, allowing the compound III to react with bromo isobutane in an organic solvent so as to obtain a suspension of a compound IV, then carrying out filtering, subjecting a filter cake to pulping with water, and carrying out filtering so as to obtain a solid compound IV; and (3) subjecting the solid compound IV prepared in the step (2) to hydrolyzing so as to obtain a Febuxostat compound I, wherein a specific reaction formula is described in the specification.
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Paragraph 0016; 0049

(2017/01/17)

Synthesis of the major metabolites of febuxostat
Total synthesis of three Febuxostat metabolites, named 67M-1, 67M-2, and 67M-4,is described in this article. Through condensation of the key intermediate compound A with different side chains, and then oxidation and hydrolysis, we obtained three target compounds with an overall yield of 19.5%-28.0%.
Li, Xiao Long,Qiu, Rui,Wan, Wei Li,Cheng, Xu,Hai, Li,Wu, Yong
p. 217 - 221
(2015/06/23)

A NOVEL PROCESS FOR THE PREPARATION OF FEBUXOSTAT
The present invention relates to a novel preparation method for 2-(3-cyano-4-isobutoxyphenyl)- 4-methyl-1,3-thiazole-5-carboxylic acid (Febuxostat) via novel and high yielded conversion of a formyl group in to a cyano group.
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Page/Page column 14

(2015/02/25)

PROCESS FOR THE PREPARATION OF 2-ARYLTHIAZOLE DERIVATIVES
The present invention relates an improved process for the preparation of 2-arylthiazole derivatives which are intermediates of Febuxostat and further conversion to Febuxostat or pharmaceutically acceptable salts thereof.
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Paragraph 0043

(2013/11/19)

AN IMPROVED PROCESS FOR THE PREPARATION OF 2-ARYLTHIAZOLE DERIVATIVES
The present invention relates an improved process for the preparation of 2- arylthiazole derivatives which are intermediates of Febuxostat and further conversion to Febuxostat or pharmaceutically acceptable salts thereof.
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Page/Page column 8

(2012/06/01)

IMPROVED PROCESS FOR THE PREPARATION OF FEBUXOSTAT
An improved and efficient process for the preparation of 2-[3-cyano-4-(2- methylpropoxy)phenyl]-4-methylthiazole-5-carboxylic acid (febuxostat) that is substantially free from amide by-product is provided.
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Page/Page column 12

(2012/02/13)

REMEDY OR PREVENTIVE FOR DIGESTIVE ULCER
An object of the present invention is to provide an agent for treating or preventing digestive ulcer that is effective even to ulcer of small intestine and others, for which gastric acid secretion inhibitors such as proton pump inhibitors are ineffective, and is superior to allopurinol in the efficaciousness and the safety. The pharmaceutical composition of the present invention comprising a non-purine xanthine oxidase inhibitor as the active ingredient is useful as an agent for treating or preventing ulcer that forms in digestive tracts by the attack of gastric acid, pepsin, stress, Helicobacter pylori bacteria, NSAID, etc. In particular, it is useful as an ulcer remedy heretofore unknown in the art as it is effective even for ulcer in small intestine for which gastric/duodenal ulcer remedies that inhibit gastric acid secretion such as proton pump inhibitors are ineffective.
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(2008/12/09)

TRIARYLCARBOXYLIC ACID DERIVATIVE
It is intended to provide an agent for treating or preventing hyperuricemia, gout, inflammatory bowel disease, diabetic nephropathy, diabetic retinopathy and so on which has a non-nucleic acid structure and exerts an excellent xanthine oxidase inhibiting action and a hypouricemic effect. It has been confirmed that a novel triarylcarboxylic acid derivative, which is characterized by having a carboxyl-substituted heteroaryl group and an aromatic ring group such as a phenyl group attached in para-position on a benzene ring and further carrying a cyano group on the same benzene ring, has a potent xanthine oxidase inhibiting action and a hypouricemic effect. Thus, it is found out that this compound is appropriately usable as an agent for treating or preventing hyperuricemia, gout, inflammatory bowel disease, diabetic nephropathy, diabetic retinopathy and so on.
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Page/Page column 16

(2008/12/06)