- Preparation method of benzoxaborole compound
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The invention discloses a preparation method of a benzoxaborole compound. The preparation method comprises the following steps: (1) reacting raw materials containing halogenated hydrocarbon and boric acid ester under an alkaline condition, acidifying and hydrolyzing to obtain an intermediate VI; and (2) reacting a raw material containing the intermediate VI with halogenated cyanophenyl to obtain the benzoxaborole compound. The raw materials are low in price, the preparation cost of the benzoxaborole compound is reduced, the steps of protection and de-protection of organic groups are not needed in the preparation process, the reaction process is simplified, and yield reduction caused by group protection is avoided; and meanwhile, the method is mild in reaction condition, low in equipment requirement and easy for large-scale industrial production.
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- PNO ligand containing planar chiral ferrocene and application thereof
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The invention discloses a PNO ligand containing planar chiral ferrocene and application thereof. The PNO ligand containing planar chiral ferrocene is a planar chiral ferrocene-containing and phenol-containing PNO ligand as shown in a general formula (I) or (II) which is described in the specification, or a planar chiral ferrocene-containing and aryl-phosphoric-acid-containingPNO ligand containing as shown in a general formula (III) or (IV) which is described in the specification, or a planar chiral ferrocene-containing and carbon-chiral-phenol-containingPNO ligand as shown in a general formula (V) or (VI) which is described in the specification. The invention provides tridentate PNO ligands and processes for their complexation with transition metal salts or transition metal complexes; the introduction of salicylaldehyde and derivatives thereof, which are simple and easy to obtain, enables the ligands to have a bifunctionalization effect, and -OH in a formed catalyst has stronger acidity and is beneficial to combination with N/O in polar double bonds. Therefore, due to the bifunctionalization effect of the catalyst, the interaction between the catalyst and a substrate can be greatly improved, so a reaction can obtain higher catalytic activity and stereoselectivity.
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Paragraph 0114-0118
(2021/06/21)
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- INTERMEDIATES AND PROCESS FOR THE PREPARATION OF A CRYSTALLINE FORM OF A TOPICAL ANTI-INFLAMMATORY AGENT
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The present invention relates to a process for the preparation of an inhibitor of phosphodiesterase 4, in particular of phosphodiesterase 4B (PDE4B), and intermediates useful for its preparation.
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Paragraph 0148
(2019/08/20)
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- A substituted boron-containing compounds and pharmaceutical compositions containing the compounds (by machine translation)
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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
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Paragraph 0128; 0130; 0131; 0132; 0133
(2019/02/02)
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- PROCESS FOR THE PREPARATION OF CRISABOROLE
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The present invention relates to a process for the preparation of crisaborole of formula (I): by preparing intermediates of formulas (II) and (III):
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Paragraph 0039-0042
(2019/07/10)
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- IRIDIUM-BASED CATALYSTS FOR HIGHLY EFFICIENT DEHYDROGENATION AND HYDROGENATION REACTIONS IN AQUEOUS SOLUTION AND APPLICATIONS THEREOF
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A series of iridium-based catalysts for dehydrogenation of formic acid, and hydrogenation using formic acid as the hydrogen source, and the process using the catalyst(s) to produce hydrogen gas from formic acid solution, or to reduce aldehydes using formic acid, are disclosed and claimed. More specifically, the present invention relates to a group of pentamethylcyclopentadienyl (Cp*) iridium complexes with different Ν,Ν-bidentate ligands that catalyze dehydrogenation from formic acid, and chemo-selective hydrogenation of aldehydes, in the aqueous solution system in a highly efficient, and long life-time manner.
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Page/Page column 13; 15
(2018/11/22)
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- Preparation method of boracic micromolecule
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The invention discloses a preparation method of a boracic micromolecule 5-(4-cyanophenoxyl)-1,3-dihydro-1-hydroxy-2,1-benzodioxole. The preparation method includes the steps of (1) subjecting 2-bromine-5-hydroxybenzaldehyde to reduction reaction in solvent with the presence of reducing agents to obtain 2-bromine-5-hydroxybenzyl alcohol; (2) subjecting 2-bromine-5-hydroxybenzyl alcohol and a hydroxyl protection reagent to reaction in solvent with the presence of alkali; (3) subjecting the previous reactant to borate reaction in solvent under an alkaline condition; (4) removing hydroxyl protecting groups from the previous reactant to obtain a benzo[c][1,2]heterocyclopentadiene-1,5(3H)-glycol body; (5) subjecting the previous reactant to reaction in solvent under an alkaline condition to obtain a target object. The preparation method has the advantages of low cost of technological raw materials, easiness in obtaining of the technological raw materials, remarkably improved reaction yield,simplicity in operation, low cost and applicability to industrial production.
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Paragraph 0058-0060
(2018/12/14)
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- PROCESS FOR THE PREPARATION OF 5-(4-CYANOPHENOXY)-1,3-DIHYDRO-1-HYDROXY-[2,1]-BENZOXABOROLE AND POLYMORPHS THEREOF
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The present invention relates to process for the preparation of 5-(4-cyano phenoxy)-1,3-dihydro-1-hydroxy-[2, 1]-benzoxaborole represented by the following structural formula- 1 and polymorphs thereof. The present invention also relates to salts of 5-(4-cyano phenoxy)-1,3-dihydro-1-hydroxy-[2,1]-benzoxaborole and process for their preparation and their use in the preparation of pure compound of the formula- 1.
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Page/Page column 20
(2018/12/13)
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- Iridium-catalyzed highly efficient chemoselective reduction of aldehydes in water using formic acid as the hydrogen source
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A water-soluble highly efficient iridium catalyst is developed for the chemoselective reduction of aldehydes to alcohols in water. The reduction uses formic acid as the traceless reducing agent and water as a solvent. It can be carried out in air without the need for inert atmosphere protection. The products can be purified by simple extraction without any column chromatography. The catalyst loading can be as low as 0.005 mol% and the turn-over frequency (TOF) is as high as 73 800 mol mol-1 h-1. A wide variety of functional groups, such as electron-rich or deficient (hetero)arenes and alkenes, alkyloxy groups, halogens, phenols, ketones, esters, carboxylic acids, cyano, and nitro groups, are all well tolerated, indicating excellent chemoselectivity.
- Yang, Zhanhui,Zhu, Zhongpeng,Luo, Renshi,Qiu, Xiang,Liu, Ji-Tian,Yang, Jing-Kui,Tang, Weiping
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supporting information
p. 3296 - 3301
(2017/07/28)
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- Boron-Containing Small Molecules as Anti-Inflammatory Agents
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Compounds and methods of treating anti-inflammatory conditions are disclosed.
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Paragraph 0702-0703
(2015/11/16)
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- Synthesis of novel structurally simplified estrogen analogues with electron-donating groups in ring A
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A library of 25 novel estrogen analogues were prepared in five to eight steps from mostly commercially available substituted anisoles via bromination, formylation, Corey-Fuchs reaction, elimination, and Sonogashira reaction. Georg Thieme Verlag Stuttgart.
- Tietze, Lutz F.,Vock, Carsten A.,Krimmelbein, Ilga K.,Nacke, Linda
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experimental part
p. 2040 - 2060
(2009/12/27)
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- 2-Alkynyl-and 2-alkenyl-pyrazolo-[4,3-e]-1,2,4-triazolo-[1,5-c]-pyrimidine adenosine A2a receptor antagonists
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Compounds having the structural formula I or a pharmaceutically acceptable salt thereof, wherein R is R1, R2, R3, R4 and R5 are H, alkyl or alkoxyalkyl; R6 is H, alkyl, hydroxyalkyl or —CH2F; R7, R8 and R9 are H, alkyl, alkoxy, alkylthio, alkoxyalkyl, halo or —CF3; and Z is optionally substituted aryl, heteroaryl or heteroaryl-alkyl are disclosed. Also disclosed is the use of compounds of formula I in the treatment of central nervous system diseases, in particular Parkinson's disease, alone or in combination with other agents for treating Parkinson's disease, and pharmaceutical compositions comprising them.
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