- Preparation method of 1-hydroxymethylcyclopropyl acetonitrile
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The present invention relates to a method for preparing 1-hydroxymethylcyclopropyl acetonitrile, which belongs to the field of pharmaceutical intermediate synthesis technology. The present invention takes pentaerythritol as raw material, after bromination reaction to give tribromo neoamyl alcohol, and then by acetylation reaction to give 3-bromo-2,2-bis (bromomethyl) propyl acetate, the starting material is selected pentaerythritol, the reaction temperature is reduced from 90 ° C to 50 ° C, the reaction time is shortened from about 35 hours to about 10 hours, shortening the reaction time, reducing the reaction temperature, greatly reducing the production cost; the use of bromine-containing materials in the reaction process, to achieve the recovery of bromine elements, greatly reducing the output of waste, At the same time, it also solves the problem that cyclopropyl dimethylol contains two hydroxyl groups, only one hydroxyl group needs to be protected; further, the present invention uses a cyanide solution instead of a cyanide solid, reducing the risk of direct contact between the operator and the cyanide-containing material. The raw materials used in the present invention are simple and readily available, the process flow is simple, suitable for industrial large-scale production.
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- Montelukast side chain intermediate and preparing method thereof
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The invention belongs to the field of medical chemistry, and particularly relates to a montelukast side chain intermediate and a preparing method thereof. A provided intermediate compound is 6-halogenated methyl-5,7-dioxaspiro[2,5] octane, wherein 1,1-cyclopropyl dimethyl carbinol serving as a starting material and 2-halogeno-1,1-dimethoxyethane are subjected to a transacetalation reaction under solid acid catalysis to obtain 6-halogenated methyl-5,7-dioxaspiro[2,5] octane, the intermediate is treated with organic alkali and then hydrolyzed with a water solution containing acetic acid to obtain monoacetylated protected diol. The problems that monoacetylated protected diol is poor in selectivity, and diol loss is serious are solved, the availability of the raw materials is improved, and the montelukast side chain intermediate can be synthesized economically and conveniently.
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- SPIROPYRROLIDINES AS MDM2 INHIBITORS
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Described are spiropyrrolidines (I) useful as inhibitors of MDM2/p53 interactions and provides useful agents for the treatment of diseases like cancer and retinal macular degeneration diseases. The invented compounds herein have the general Further described are pharmaceutical compositions that comprise one or more compounds of the invention, a pharmaceutically acceptable salt or pro-drug and/or a pharmaceutically acceptable carrier or excipient.
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Paragraph 0237-0238
(2015/11/30)
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- PREPARATION OF MONTELUKAST AND ITS SALTS
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There is provided a process for the preparation of montelukast of the Formula (I).
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Page/Page column 36
(2008/12/05)
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- Process for preparation of [1-(mercaptomethyl)cyclopropyl]acetic acid and related derivatives
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The present invention provides a novel process for preparing [1-(mercaptomethyl)cyclopropyl]acetic acid with high purity and related derivatives.
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Page/Page column 7
(2008/06/13)
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- Process for making montelukast and intermediates therefor
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A process for making montelukast, a pharmaceutically useful compound of the following formula and salts thereof: using a compound of formula (20) is provided.
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Page/Page column 10
(2008/06/13)
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- ARYL SULFONAMIDE COMPOUNDS AND USES RELATED THERETO
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The present invention provides Aryl Sulfonamide Compounds having the formula: (I); and prodrugs or pharmaceutically acceptable salts or prodrugs thereof. The Aryl Sulfonamide Compounds are useful for treating diabetes, obesity, and other diseases and disorders.
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Page/Page column 69-70
(2010/02/12)
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- Process for the preparation of leukotriene anatgonists
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The present invention relates to a process for the preparation of a compound of formula (I) or a sodium salt thereof STR1 wherein HET is 7-chloroquinolin-2-yl or 6,7-difluoroquinolin-2-yl, which comprises: reacting the dilithium dianion of 1-(mercaptomethyl)cyclopropaneacetic acid with a compound of formula (II) STR2 wherein HET is as defined above and L is arylsulfonyl or alkylsulfonyl. The invention further provides the dicyclohexylamine salt of a compound of formula (I).
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- Preparation of cyclic sulfites by transesterification of diols and diisopropyl sulfite
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Cyclic sulfites of 1,2-, 1,3- and 1,4-diols can be prepared in high yield by acid or base catalyzed transesterification with diisopropyl sulfite.
- King, Steven A.,Pipik, Brenda,Conlon, David A.,Bhupathy
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p. 701 - 707
(2007/10/03)
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- Process for the preparation of 1-(thiomethyl)-cyclopropaneacetic acid
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The present invention provides a novel process for the preparation of 1,1-cyclopropanedimethanol cyclic sulfite which comprises: (a) contacting 1,1-cyclopropanedimethanol with dialkylsulfite in the presence of a base; and (b) removing from the reaction mixture the alcohol reaction by-product. This process is incorporated in the additional novel processes for preparing 1-(hydroxymethyl)cyclopropaneacetonitrile and 1-(thiomethyl)cyclopropaneacetic acid.
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- PYRIDINE-SUBSTITUTED BENZYL ALCOHOLS AS LEUKOTRIENE ANTAGONISTS
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Compounds having the formula I: STR1 are antagonists of the actions of leukotrienes. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents. They are also useful in treating angina, cerebral spasm, glomerular nephritis, hepatitis, endotoxemia, uveitis, and allograft rejection.
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- HETEROARYL AND HALOARYL QUINOLINE DERIVATIVES OF CYCLOPROPANEACETIC ACID AS LEUKOTRIENE ANTAGONISTS
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Compounds having the formula I: STR1 are antagonists of the actions of leukotrienes. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents. They are also useful in treating angina, cerebral spasm, glomerular nephritis, hepatitis, endotoxemia, uveitis, and allograft rejection.
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- DIARYL 5,6-FUSED HETEROCYCLIC ACIDS AS LEUKOTRIENE ANTAGONISTS
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Compounds having the formula I: STR1 are antagonists of the actions of leukotrienes. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents. They are also useful in treating angina, cerebral spasm, glomerular nephritis, hepatitis, endotoxemia, uveitis, and allograft rejection.
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- AZA-5,5-FUSED HETROCYCLIC ACIDS AS LEUKOTRIENE ANTAGONISTS
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Compounds having the formula I: STR1 are antagonists of the actions of leukotrienes. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents. They are also useful in treating angina, cerebral spasm, glomerular nephritis, hepatitis, endotoxemia, uveitis, and allograft rejection.
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- Fluorinated hydroxyalkylquinoline acids as leukotriene antagonists
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Compounds having the formula I: STR1 are leukotriene antagonists and inhibitors of leukotriene biosynthesis. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents. They are also useful in treating angina, cerebral spasm, glomerular nephritis, hepatitis, endotoxemia, uveitis, and allograft rejection.
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