cas 107496-54-8, 3,3-Difluorocyclobutanecarboxylic acid

Articles about 107496-54-8Total 19 be found

A practical synthesis of 3,3-difluorocyclobutane carboxylic acid
We reported a straightforward, three step synthesis of 3,3- difluorocyclobutane carboxylic acid.
Elend, Dirk,Fengas, David,Fray, M. Jonathan
p. 657 - 662
(2005)
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JAK INHIBITORS
Disclosed is a series of JAK inhibitors, which specifically relates to a compound shown in formula (I) or pharmaceutically acceptable salts thereof.
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(2018/05/03)

Multigram Synthesis of C 4/C5 3,3-Difluorocyclobutyl-Substituted Building Blocks
An approach for the multigram synthesis of 3,3-difluorocyclobutyl-substituted building blocks (including carboxylic acid, amines, alcohols, azide, trifluoroborate ketone) is described. It is shown that, in most cases, ethyl 3,3-difluorocyclobutanecarboxylate is a convenient common synthetic intermediate to obtain the target derivatives. For preparation of 3,3-difluorocyclobutanol or -cyclobutanone, an alternative pathway via reaction of dichloroketene and tert -butyl or benzyl vinyl ether should be applied.
Melnykov, Kostiantyn P.,Granat, Dmitriy S.,Volochnyuk, Dmitriy M.,Ryabukhin, Sergey V.,Grygorenko, Oleksandr O.
p. 4949 - 4957
(2018/12/13)

Method for synthesizing 3,3-difluorocyclobutanoic acid
The invention provides a method for synthesizing 3,3-difluorocyclobutanoic acid. The method specifically comprises the following steps: taking 3-oxocyclobutane formate as a starting raw material, obtaining 3,3-difluorocyclobutanoic acid through generating difluoro-substituted reaction with a fluorinated reagent BAST, generating saponification hydrolysis with alkali and acidifying to obtain the 3,3-difluorocyclobutanoic acid. The method provided by the invention has the advantages of being short in reaction route, stable and safe in raw material performance, mild in reaction condition and suitable for industrial production.
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Paragraph 0015

(2018/10/19)

Substituted pyrazolo-piperazines as casein kinase 1 δ/ε inhibitors
The invention provides compounds of Formula (I): and pharmaceutically acceptable salts thereof. The compounds of Formula (I) inhibit protein kinase activity thereby making them useful as anticancer agents.
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Page/Page column 337; 338

(2016/03/19)

Novel process for synthesizing 3, 3-difluorocyclobutyric acid
The invention provides a novel process for synthesizing 3, 3-difluorocyclobutyric acid. No fluorinating reagent like DAST is used, and the novel process is realized directly through three-step reaction, thereby being low in production cost and suitable for industrial production. The novel process has the advantages that yield is increased, and cost is lowered greatly; strong-acid hydrolysis of cyan is omitted, so that yield is increased, cost is lowered, and 'three wastes' are reduced; hydrogenation condition is changed, and original high-pressure reaction is changed into low-pressure reaction, so that reaction dangerousness is reduced, cost is lowered, and yield is increased.
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Paragraph 0047-0050

(2017/04/20)

3,3-gem-difluoro cyclobutanecarboxylic acid industrial preparation method
The invention relates to a 3,3-gem-difluoro cyclobutanecarboxylic acid industrial preparation method. The method mainly solves the technical problem of existing preparing methods that the price of the raw material 3-oxo-cyclobutylcarboxylic acid or 3-meth
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Paragraph 0013

(2016/10/17)

THERAPEUTICALLY ACTIVE COMPOUNDS AND THEIR METHODS OF USE
Provided are methods of treating a cancer characterized by the presence of a mutant allele of IDH1/2 comprising administering to a subject in need thereof a compound described here.
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(2015/02/19)

THERAPEUTICALLY ACTIVE COMPOUNDS AND THEIR METHODS OF USE
Provided are methods of treating a cancer characterized by the presence of a mutant allele of IDH1/2 comprising administering to a subject in need thereof a compound described here.
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(2015/03/31)

THERAPEUTICALLY ACTIVE COMPOUNDS AND USE THEREOF
Provided are therapeutically active compounds and the use in manufacture of medicaments for treating a cancer characterized by the presence of a mutant allele of IDH1.
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(2015/02/19)

THERAPEUTICALLY ACTIVE COMPOUNDS AND THEIR METHODS OF USE
Provided are methods of treating a cancer characterized by the presence of a mutant allele of IDH1/2 comprising administering to a subject in need thereof a compound described here.
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(2015/02/19)

THERAPEUTICALLY ACTIVE COMPOSITIONS AND THEIR METHODS OF USE
Provided are methods of treating a cancer characterized by the presence of a mutant allele of IDH1/2 comprising administering to a subject in need thereof a compound described here.
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(2013/07/31)

THERAPEUTICALLY ACTIVE COMPOUNDS AND THEIR METHODS OF USE
Provided are methods of treating a cancer characterized by the presence of a mutant allele of IDH1/2 comprising administering to a subject in need thereof a compound described here.
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(2013/07/31)

THERAPEUTICALLY ACTIVE COMPOUNDS AND THEIR METHODS OF USE
Provided are methods of treating a cancer characterized by the presence of a mutant allele of IDH1/2 comprising administering to a subject in need thereof a compound described here.
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(2013/07/31)

Discovery of novel HCV inhibitors: Synthesis and biological activity of 6-(indol-2-yl)pyridine-3-sulfonamides targeting hepatitis C virus NS4B
A novel series of 6-(indol-2-yl)pyridine-3-sulfonamides was prepared and evaluated for their ability to inhibit HCV RNA replication in the HCV replicon cell culture assay. Preliminary optimization of this series furnished compounds with low nanomolar potency against the HCV genotype 1b replicon. Among these, compound 8c has identified as a potent HCV replicon inhibitor (EC50 = 4 nM) with a selectivity index with respect to cellular GAPDH of more than 2500. Further, compound 8c had a good pharmacokinetic profile in rats with an IV half-life of 6 h and oral bioavailability (F) of 62%. Selection of HCV replicon resistance identified an amino acid substitution in HCV NS4B that confers resistance to these compounds. These compounds hold promise as a new chemotype with anti-HCV activity mediated through an underexploited viral target.
Zhang, Xiaoyan,Zhang, Nanjing,Chen, Guangming,Turpoff, Anthony,Ren, Hongyu,Takasugi, James,Morrill, Christie,Zhu, Jin,Li, Chunshi,Lennox, William,Paget, Steven,Liu, Yalei,Almstead, Neil,George Njoroge,Gu, Zhengxian,Komatsu, Takashi,Clausen, Valerie,Espiritu, Christine,Graci, Jason,Colacino, Joseph,Lahser, Fred,Risher, Nicole,Weetall, Marla,Nomeir, Amin,Karp, Gary M.
p. 3947 - 3953
(2013/07/27)

Compounds and Their Use for Treatment of Amyloid Beta-Related Diseases
The present invention relates to novel compounds of formula (I) and pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising said compounds, processes for making said compounds, and their use as medicaments for treatment and/or prevention of Aβ-related diseases.
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Page/Page column 40

(2012/05/21)

Triazole derivatives which are SMO antagonists
The present invention provides a method for the treatment or prevention of conditions which can be ameliorated by Smo antagonism, which method comprises administration to a patient in need thereof of an effective amount of a compound of formula I or a com
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Page/Page column 12; 13

(2008/12/04)

TRIAZOLE DERIVATIVES AS INHIBITORS OF 11-BETA-HYDROXYSTEROID DEHYDROGENASE-1
Triazole derivatives of structural formula I are selective inhibitors of the 11β-hydroxysteroid dehydrogenase-1. The compounds are useful for the treatment of diabetes, such as noninsulin-dependent diabetes (NIDDM), hyperglycemia, obesity, insulin resista
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Page/Page column 24

(2008/06/13)