Patent classifications
C07C303/26
NORMAL PARAFFIN COMPOSITION
The present invention relates to a normal paraffin composition comprising from 45 to 60 wt. % of a fraction of normal paraffin having from 10 to 13 carbon atoms and from 40 to 55 wt. % of a fraction of normal paraffin having from 14 to 18 carbon atoms.
QUINOLINE COMPOUND SALT OR CRYSTAL FORM, PREPARATION METHOD THEREFOR, AND APPLICATION THEREOF
The present invention relates to the field of biomedicine; provided are a quinoline compound salt or a crystal form thereof, a preparation method therefor and an application thereof. The quinoline compound is as shown in Formula (I), and the provided salt may be used as an inhibitor of phosphoinositide 3-kinase for the treatment of diseases related to phosphoinositide 3-kinase. More particularly, the compound of Formula (I) may be 2,4-diamino-6-[1-(7-fluoro-2-pyridin-2-yl-quinolin-3-yl)-ethylamino]-pyrimidine-5-carbonitrile (Compound A), the structure thereof being as shown below. Crystal form I of p-toluenesulfonate of the compound may be used as an inhibitor of phosphoinositide 3-kinase for the treatment of diseases related to phosphoinositide 3-kinase.
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QUINOLINE COMPOUND SALT OR CRYSTAL FORM, PREPARATION METHOD THEREFOR, AND APPLICATION THEREOF
The present invention relates to the field of biomedicine; provided are a quinoline compound salt or a crystal form thereof, a preparation method therefor and an application thereof. The quinoline compound is as shown in Formula (I), and the provided salt may be used as an inhibitor of phosphoinositide 3-kinase for the treatment of diseases related to phosphoinositide 3-kinase. More particularly, the compound of Formula (I) may be 2,4-diamino-6-[1-(7-fluoro-2-pyridin-2-yl-quinolin-3-yl)-ethylamino]-pyrimidine-5-carbonitrile (Compound A), the structure thereof being as shown below. Crystal form I of p-toluenesulfonate of the compound may be used as an inhibitor of phosphoinositide 3-kinase for the treatment of diseases related to phosphoinositide 3-kinase.
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METHOD FOR PRODUCING 1,1'-BINAPHTHYL DERIVATIVES AND 1,1'-BINAPHTHYL DERIVATIVES
In a production method of the present disclosure, a 1,1-binaphthyl precursor derivative, an organic acid, and an iodinating or brominating agent are mixed. The 1,1-binaphthyl precursor derivative has a 1,1-binaphthyl skeleton and has an electron-donating group at the 2-position of the 1,1-binaphthyl skeleton and at the 2-position of the 1,1-binaphthyl skeleton, and the electron-donating group contains an oxygen atom directly bonded to the skeleton. With the production method of the present disclosure, a 1,1-binaphthyl derivative having a substituent introduced at the 8-position and/or 8-position of the 1,1-binaphthyl skeleton can be obtained. The 1,1-binaphthyl derivative obtained by the production method of the present disclosure can be a compound further having a substituent introduced at at least one position selected from the 4-position, 4-position, 5-position, 5-position, 6-position, and 6-position of the 1,1-binaphthyl skeleton.
METHOD FOR PRODUCING 1,1'-BINAPHTHYL DERIVATIVES AND 1,1'-BINAPHTHYL DERIVATIVES
In a production method of the present disclosure, a 1,1-binaphthyl precursor derivative, an organic acid, and an iodinating or brominating agent are mixed. The 1,1-binaphthyl precursor derivative has a 1,1-binaphthyl skeleton and has an electron-donating group at the 2-position of the 1,1-binaphthyl skeleton and at the 2-position of the 1,1-binaphthyl skeleton, and the electron-donating group contains an oxygen atom directly bonded to the skeleton. With the production method of the present disclosure, a 1,1-binaphthyl derivative having a substituent introduced at the 8-position and/or 8-position of the 1,1-binaphthyl skeleton can be obtained. The 1,1-binaphthyl derivative obtained by the production method of the present disclosure can be a compound further having a substituent introduced at at least one position selected from the 4-position, 4-position, 5-position, 5-position, 6-position, and 6-position of the 1,1-binaphthyl skeleton.
SYNTHESIS OF HYPERVALENT IODINE REAGENTS WITH DIOXYGEN
Methods of synthesis of hypervalent iodine reagents and methods for oxidation of organic compounds are disclosed.
SYNTHESIS OF HYPERVALENT IODINE REAGENTS WITH DIOXYGEN
Methods of synthesis of hypervalent iodine reagents and methods for oxidation of organic compounds are disclosed.
Compositions and methods for sulfation of carbohydrates and peptides via electron-deficient aryl sulfate diesters
In one aspect, the disclosure relates to a facile strategy to introduce electron-deficient aryl sulfate diesters to silylated hydroxyl groups of carbohydrates and amino acids, among other substrates, wherein selective hydrolysis and the removal of an electron-deficient aromatic group allows for the efficient generation of sulfated carbohydrates, peptides, and other compounds. The incorporation of electron-deficient aryl sulfate diesters in the early stage of the synthesis of glycans, peptides, and the like, disclosed herein avoids time-consuming protecting group manipulations, simplifies the purification of sulfated products, and improves the overall yield and efficiency. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present disclosure.
Compositions and methods for sulfation of carbohydrates and peptides via electron-deficient aryl sulfate diesters
In one aspect, the disclosure relates to a facile strategy to introduce electron-deficient aryl sulfate diesters to silylated hydroxyl groups of carbohydrates and amino acids, among other substrates, wherein selective hydrolysis and the removal of an electron-deficient aromatic group allows for the efficient generation of sulfated carbohydrates, peptides, and other compounds. The incorporation of electron-deficient aryl sulfate diesters in the early stage of the synthesis of glycans, peptides, and the like, disclosed herein avoids time-consuming protecting group manipulations, simplifies the purification of sulfated products, and improves the overall yield and efficiency. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present disclosure.
Method for manufacturing cyclopropane compound
The present invention provides an industrially advantageous production method of (1R,2S)-2-{[((2,4-dimethylpyrimidin-5-yl)oxy}methyl]-2-(3-fluorophenyl)-N-(5-fluoropyridin-2-yl)cyclopropane-1-carboxamide. (1R,2S)-2-{[((2,4-Dimethylpyrimidin-5-yl)oxy}methyl]-2-(3-fluorophenyl)-N-(5-fluoropyridin-2-yl)cyclopropane-1-carboxamide (compound [A]) is produced by an industrially advantageous method by a route via a novel compound. ##STR00001##
wherein each symbol is as described in the description.