906673-54-9Relevant academic research and scientific papers
Preparation method of 5-(4-cyanophenoxy)-2, 3-dihydro-1-hydroxy-2, 1-benzoxaborole intermediate
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, (2019/11/04)
The invention discloses a preparation method of 5-(4-cyanophenoxy)-2, 3-dihydro-1-hydroxy-2, 1-benzoxaborole intermediate. The 5-(4-cyanophenoxy)-2, 3-dihydro-1-hydroxy-2, 1-benzoxaborole intermediatecomprises a structure as shown in a formula IV. The pre
A substituted boron-containing compounds and pharmaceutical compositions containing the compounds (by machine translation)
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Paragraph 0116; 0118; 0119; 0120; 0121, (2019/02/02)
The present invention provides a substituted boron-containing compounds and containing the compound of the pharmaceutical composition and its use, the boron-containing compound of the formula (I) compounds, or their pharmaceutically acceptable salt, prodr
Synthesizing method of 4-(4-bromo-3-aldehyde-phenoxyl)-benzonitrile
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, (2019/01/14)
The invention provides a synthesizing method of 4-(4-bromo-3-aldehyde-phenoxyl)-benzonitrile. The synthesizing method comprises the following steps of using 3-methylphenol as the starting raw material, and reacting with acid anhydride to prepare 3-methyl-benzene ester; enabling the 3-methyl-benzene ester and sulfonyl chloride to react, so as to prepare a mixture of 3-chloromethyl-benzene ester and3-dichloromethyl-benzene ester; adding ulotropine, and hydrolyzing, so as to obtain 3-hydroxyl-benzaldehyde; performing brominating reaction, so as to obtain 4-bromo-3-hydroxyl-benzaldehyde; adding 4-fluorobenzonitrile, and performing condensation reaction, so as to obtain the 4-(4-bromo-3-aldehyde-phenoxyl)-benzonitrile. The synthesizing method has the advantages that the prices of the reactionraw materials are low, the obtaining is easy, the reaction steps are fewer, the production cost is low, the technology is simple, the product purity is high and reaches 99.0% or above, and the synthesizing method is suitable for industrialized production.
PROCESS FOR PREPARING 4-[(1-HYDROXY-1,3-DIHYDRO-2,1-BENZOXABOROL-5-YL)OXY]BENZONITRILE (CRISABOROLE)
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Paragraph 0120, (2018/07/22)
The present invention relates to a new one-pot synthesis employing 4-(4-bromo-3-(hydroxymethyl)phenoxy)benzonitrile (compound B) for preparing (4-[(1-hydroxy-1,3-dihydro-2,1-benzoxaborol-5-yl)oxy]benzonitrile (crisaborole) and pharmaceutically acceptable salts thereof in high yield and high purity. The novel process of the present invention is particularly suitable for industrial scale manufacture of crisaborole and its salts with excellent purity and good yields. The present invention also describes an intermediate, 4-(3-formyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)phenoxy)benzonitrile (compound I), which is inter alia suitable for preparing (4-[(1-hydroxy-1,3-dihydro-2, 1-benzoxaborol-5-yl)oxy]benzonitrile (crisaborole) and pharmaceutically acceptable salts thereof, as well as a another process suitable for industrial scale applications, employing the intermediate compound I in the preparation of crisaborole and pharmaceutically acceptable salts thereof, in high yield and high purity.
PROCESS FOR PREPARATION OF CRISABOROLE
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Paragraph 0167; 0181, (2019/01/06)
The present invention relates to a process for the preparation of crisaborole, the process comprising reacting a compound of formula IIa with a compound of formula III to give a compound of formula IV and converting the compound of formula IV to crisaborole. The present invention also relates to a process for the preparation of crystalline crisaborole.
Discovery and structure-activity study of a novel benzoxaborole anti-inflammatory agent (AN2728) for the potential topical treatment of psoriasis and atopic dermatitis
Akama, Tsutomu,Baker, Stephen J.,Zhang, Yong-Kang,Hernandez, Vincent,Zhou, Huchen,Sanders, Virginia,Freund, Yvonne,Kimura, Richard,Maples, Kirk R.,Plattner, Jacob J.
scheme or table, p. 2129 - 2132 (2009/12/07)
A series of phenoxy benzoxaboroles were synthesized and screened for their inhibitory activity against PDE4 and cytokine release. 5-(4-Cyanophenoxy)-2,3-dihydro-1-hydroxy-2,1-benzoxaborole (AN2728) showed potent activity both in vitro and in vivo. This compound is now in clinical development for the topical treatment of psoriasis and being pursued for the topical treatment of atopic dermatitis.
Survivin inhibitors
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Page/Page column 20, (2010/11/26)
Compounds that inhibit survivin, compositions containing the compounds and methods of treating diseases in which survivin is unregulated or overexpressed are disclosed.
