1081-30-7Relevant academic research and scientific papers
Isoxazoles from 1,1-disubstituted bromoalkenes
Dadiboyena, Sureshbabu,Xu, Jianping,Hamme II, Ashton T.
, p. 1295 - 1298 (2007)
The regioselective synthesis of 3,5-disubstituted isoxazoles was achieved through the 1,3-dipolar cycloaddition of nitrile oxides with 1,1-disubstituted bromoalkenes. The substituted bromoalkenes function as alkyne synthons which were used to construct 5,
Hypervalent iodine mediated synthesis of di- and tri-substituted isoxazoles via [3+2] cycloaddition of nitrile oxides
Singhal, Ankur,Parumala, Santosh Kumar Reddy,Sharma, Arun,Peddinti, Rama Krishna
, p. 719 - 722 (2016)
An efficient and rapid protocol for the synthesis of 3,4-disubstituted and 3,4,5-trisubstituted isoxazoles under catalyst-free conditions is described. This protocol involves pre-oxidation of aldoxime into nitrile oxide using diacetoxyiodobenzene. The in
Methyl 3-Substituted-isoxazole-5- Carboxylates syntheses on solid supports via wang resin-bound 2,3-dibromopropionate
Sheng, Shou-Ri,He, Ai-Ying,Wei, Mei-Hong,Zhu, Ai-Li,Cai, Ming-Zhong
, p. 444 - 448 (2012)
A novel Wang resin-bound 2,3-dibromopropionate reagent has been developed and used as a potential dipolarophile for the facile preparation of methyl 3-substituted-isoxazole-5-carboxylates through triethylamine, promoting a sequence of reactions involving the in situ generation of 2-bromoacrylate resin and nitrile oxide, regioselective 1,3-dipolar cycloaddition, and loss of hydrogen bromide in one pot, and then cleavage from the resin with sodium methoxide. The advantages of this method include simple operation and mild conditions with good yield and high purity of the products. Copyright
COMPOUNDS, COMPOSITIONS AND METHODS OF INCREASING CFTR ACTIVITY
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Paragraph 0245, (2017/02/24)
The present disclosure features compounds such as those having the Formulae (I) and (II), which can increase cystic fibrosis transmembrane conductance regulator (CFTR) activity as measured in human bronchial epithelial (hBE) cells. The present disclosure also features methods of treating a condition associated with decreased CFTR activity or a condition associated with a dysfunction of proteostasis comprising administering to a subject an effective amount of a disclosed compound, such as a compound of Formula (I) or (II).
METHODS OF TREATING PULMONARY DISEASES AND DISORDERS
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Paragraph 0245, (2017/07/14)
The present disclosure features disclosed method of treating disorders such as COPD, bronchitis and/or asthma using disclosed compounds, optionally together with one or more additional active agents. Contemplated methods include administrating orally or by inhalation to a patient one or more disclosed compounds.
COMPOUNDS, COMPOSITIONS, AND METHODS FOR INCREASING CFTR ACTIVITY
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Paragraph 0271, (2016/07/27)
The present disclosure is directed to disclosed compounds that increase cystic fibrosis transmembrane conductance regulator (CFTR) activity as measured in human bronchial epithelial (hBE) cells.
ISOXAZOLE COMPOUNDS AND METHODS FOR THE TREATMENT OF CYSTIC FIBROSIS
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Page/Page column 45; 46, (2016/04/26)
The invention relates to a compound of Formula (I) and methods of treating cystic fibrosis comprising the step of administering a therapeutically effective amount of a compound of Formula (I) or II to a patient in need thereof: Formula (I) and Formula (II). The invention relates to the use of substituted oxazole and substituted thiazole compounds in the treatment of cystic fibrosis transmembrane conductance regulator (CFTR) mediated diseases.
An environmentally benign synthesis of isoxazolines and isoxazoles mediated by potassium chloride in water
Han, Liuquan,Zhang, Bijun,Zhu, Min,Yan, Jie
supporting information, p. 2308 - 2311 (2014/04/17)
An effective and environmentally benign procedure for the synthesis of isoxazolines and isoxazoles has been developed by a cycloaddition of nitrile oxides with alkenes or alkynes in water. In this approach, potassium chloride is first oxidized into chlorine in water by the environmentally friendly oxidant Oxone, then aldoximes are oxidized into nitrile oxides by the in situ generated hypochlorous acid, finally a 1,3-dipolar cycloaddition between nitrile oxides and alkenes or alkynes occurs to provide the corresponding isoxazolines and isoxazoles in good yields.
Solid-phase organic synthesis of methyl isoxazole-5-carboxylates based on wang resin-bound 1-phenylselenoacrylate
Tang, Ni,Sheng, Shou-Ri,Hu, Qiao-Sheng,Qu, Hong-En,Cai, Ming-Zhong
experimental part, p. 3279 - 3287 (2012/09/08)
A novel Wang resin-bound 1-phenylselenoacrylate reagent has been developed and used as dipolarophile for the 1,3-dipolar cycloaddition with nitrile oxides to the regioselective synthesis of methyl 3-substituted isoxazole-5-carboxylates in good yields and
Generation of nitrile oxides from oximes using t -BuOI and their cycloaddition
Minakata, Satoshi,Okumura, Sota,Nagamachi, Toshiki,Takeda, Youhei
supporting information; experimental part, p. 2966 - 2969 (2011/07/07)
tert-Butyl hypoiodite (t-BuOI) was found to be a powerful reagent for the cycloaddition of oximes and alkenes/alkynes, leading to the formation of a variety of isoxazolines or isoxazoles under mild conditions.
