Abstract: Novel synthetic routes, which are highly applicable for industrial preparation of therapeutically beneficial oxidized phospholipids are disclosed. Particularly, novel methods for efficiently preparing compounds having a glycerolic backbone and one or more oxidized moieties attached to the glycerolic backbone, which are devoid of column chromatography are disclosed. Further disclosed are novel methods of introducing phosphorous-containing moieties such as phosphate moieties to compounds having glycerolic backbone and intermediates formed thereby.
Abstract: Phosphate ester compounds are prepared by reacting phosphoryl chloride with at least one mono(alkylene glycol) monoether or poly(alkylene glycol) monoether, or a mixture at least one mono(alkylene glycol) monoether or poly(alkylene glycol) monoether and at least one alkylene glycol or polyalkylene glycol, in the presence of at least three moles per mole of phosphoryl chloride of a pyridinyl compound that is devoid of aliphatic nitrogen atoms.
Abstract: Novel synthetic routes, which are highly applicable for industrial preparation of therapeutically beneficial oxidized phospholipids are disclosed. Particularly, novel methods for efficiently preparing compounds having a glycerolic backbone and one or more oxidized moieties attached to the glycerolic backbone, which are devoid of column chromatography are disclosed. Further disclosed are novel methods of introducing phosphorous-containing moieties such as phosphate moieties to compounds having glycerolic backbone and intermediates formed thereby.
Abstract: The present invention relates to a process for preparation of a phosphoromonochloridite in high yield by contacting phosphorus trichloride (PCl3) with an aromatic diol in a solution of one or more organic solvents under reaction conditions sufficient to produce the phosphoromonochloridite. The reaction is carried out by adding a feed solution containing the aromatic diol dissolved in a first organic solvent into a reaction zone containing PCl3, and optionally one or more second organic solvents, the addition being conducted so as to maintain substantially isothermal process conditions. The reaction solution comprises greater than 0.01 to less than 5 mole percent of a nitrogen base.
Abstract: The present invention relates to a novel {4-[2-(dimethylamino)-1-(1-hydroxycyclohexyl)ethyl]phenoxy}phosphate or a pharmaceutically acceptable salt thereof, a production method therefor and a pharmaceutical composition for preventing and treating central nervous system disorders which contains the same as an active component. The novel {4-[2-(dimethylamino)-1-(1-hydroxycyclohexyl)ethyl]phenoxy}phosphate or a pharmaceutically acceptable salt thereof according to the present invention can beneficially be used to prevent and treat central nervous system disorders since it exhibits an equivalent biological and pharmacological activity to venlafaxine and salts thereof which are known in the field, it has very little toxicity, and, in particular, it is outstandingly soluble in water as compared with prior-art venlafaxine derivatives.
Type:
Application
Filed:
May 8, 2009
Publication date:
March 10, 2011
Applicant:
JE IL PHARMACEUTICAL CO., LTD.
Inventors:
Seok Won Kang, Jong Soo Chun, Heung Mo Kang, Eui Seok Hong, Kwang-Woo Chun, Young Seok Byun, Myung-Hwa Kim, Young II Moon, Jei Man Ryu
Abstract: The present invention relates to a method for producing an amino group-containing phosphate compound, by which the compound can be easily synthesized through a one-step reaction. The method for producing an amino group-containing phosphate compound comprises reacting an aminophenol compound represented by the general formula (1) with a dichlorophosphoric acid compound represented by the general formula (2): (where X1, X2, X3, X4 and X5 each represent a hydrogen atom or an alkyl group having 1 to 3 carbon atoms) in the presence of an inorganic basic compound in an aprotic organic solvent, to obtain a amino group-containing phosphate compound represented by the following general formula (3) where X1, X2, X3, X4 and X5 are defined in the same way as in the general formula (2).
Type:
Application
Filed:
June 9, 2006
Publication date:
November 25, 2010
Applicant:
SHOWA HIGHPOLYMER CO., LTD.
Inventors:
Hirotoshi Kamata, Kentarou Takahashi, Hui Li, Boris Ionin
Abstract: Disclosed herein is an improved process for preparing a phosphorodihalodithioate comprising reacting a mercaptan with a thiophorphoryl halide in the presence of a catalyst, the improvement comprising a catalytic amount of a tertiary amine catalyst.
Type:
Grant
Filed:
April 28, 1994
Date of Patent:
June 18, 1996
Assignee:
Bayer Corporation
Inventors:
Vidyanatha A. Prasad, Peter E. Newallis
Abstract: This invention relates to a novel process for preparing bis(aryl)phosphorohalidates which are useful in the synthesis of various enol phosphates. The process of this invention provides a means of producing a high-yield, high-purity product without the need for costly crystallization or impractical, high temperature distillations.
Abstract: To obtain an enhanced two-dimensional image of a raised, light-reflective reflective feature (12), and its lower height surrounding background such that the contrast between them is enhanced, a line of light having a gradient profile is directed at an acute angle at the feature and its background to illuminate a strip of area thereacross. The reflectance intensity of the illuminated strip will vary in accordance with the height thereof because of the gradient intensity profile of the line of light. When the line of light is spanned across the feature and its background, the resultant image of the feature and its background, captured by spanning a linescan camera (24) thereacross, will exhibit an enhanced contrast between the feature and its background because of the greater height of the feature.
Abstract: Thiophosphonate compounds having the formula ##STR1## in which R is alkyl, haloalkyl or aryl; X is chloro or SR.sub.2 ; R.sub.1 is alkyl or aryl; and when X is SR.sub.2 then R.sub.2 is a group identical to R.sub.1, or R.sub.1 and R.sub.2 taken together form an optionally alkyl-substituted polymethylene group, are prepared by reaction of a thiophosphonodichloride with a mercaptan in the presence of a catalytic amount of a quaternary ammonium or phosphonium salt, a tertiary amine or hydrohalide thereof or an alkali metal halide combined with a Crown ether, in the substantial absence of a base.
Type:
Grant
Filed:
December 12, 1988
Date of Patent:
September 11, 1990
Assignee:
ICI Americas Inc.
Inventors:
Jeffrey D. Robbins, Richard D. Gless, Jr.