- METHOD FOR PREPARING ARYL POLYOXY ALKYL QUATERNARY AMMONIUM COMPOUND
-
A method for preparation of an aryl poly(oxalkyl) quaternary ammonium compound is provided, said method comprising steps of: 1) reacting a phenol with a dihalopolyalkylene ether under the action of a phase transfer catalyst, to obtain an arylpoly(oxalkyl) halide; 2) reacting said arylpoly(oxalkyl) halide with an amination reagent under the action of a phase transfer catalyst, to obtain an arylpoly(oxalkyl) amine; 3) reacting said arylpoly(oxalkyl) amine with an alkylation reagent, to obtain an aryl poly(oxalkyl) quaternary ammonium compound; wherein R1 is H or a C1 to C16 alkyl group, located in the ortho, meta or para position; n is an integer of 2 to 6; R2 is H or a C1 to C16 alkyl group; R3 is H or a C1 to C16 alkyl group; R4 is a C1 to C16 alkyl group; X1 is Br or Cl; X is Cl, Br, or I. The preparation method according to the present invention requires low temperature and low pressure, the reaction time is short, and an overall yield can reach 75%. The operation is simple, the cost is low, and the product can be separated easily and have a purity of pharmaceutical grade, thereby facilitating the large-scale production.
- -
-
Paragraph 0050; 0051; 0052
(2014/03/25)
-
- METHOD FOR PREPARATION OF ARYL POLY(OXALKYL) QUATERNARY AMMONIUM COMPOUND
-
A method for preparation of an aryl poly(oxalkyl) quaternary ammonium compound is provided, said method comprising steps of: 1) reacting a phenol with a dihalopolyalkylene ether under the action of a phase transfer catalyst, to obtain an arylpoly(oxalkyl) halide; 2) reacting said arylpoly(oxalkyl) halide with an amination reagent under the action of a phase transfer catalyst, to obtain an arylpoly(oxalkyl) amine; 3) reacting said arylpoly(oxalkyl) amine with an alkylation reagent, to obtain an aryl poly(oxalkyl) quaternary ammonium compound; wherein R1 is H or a C1 to C16 alkyl group, located in the ortho, meta or para position; n is an integer of 2 to 6; R2 is H or a C1 to C16 alkyl group; R3 is H or a C1 to C16 alkyl group; R4 is a C1 to C16 alkyl group; X1 is Br or Cl; X is Cl, Br, or I. The preparation method according to the present invention requires low temperature and low pressure, the reaction time is short, and an overall yield can reach 75%. The operation is simple, the cost is low, and the product can be separated easily and have a purity of pharmaceutical grade, thereby facilitating the large-scale production.
- -
-
Paragraph 0065
(2014/07/08)
-
- NOVEL FORMULATION OF DEHYDRATED LIPID VESICLES FOR CONTROLLED RELEASE OF ACTIVE PHARMACEUTICAL INGREDIENT VIA INHALATION
-
A new formulation of dehydrated lipid vesicles employs a vesicle preserver and permits the control of release and delivery of active pharmaceutical ingredients into the respiratory system for treatment in particular of asthma. The typical formulation provides controlled release of the active pharmaceutical ingredient from 0% to 100% from 0 to 72 hours after inhalation, changes the systemic administration to topical administration, allows prolonged therapeutic period for one administration, increased stability, with reduced dose, reduced systemic side effects, reduced toxicity.
- -
-
-
- Substitution reactions of benzethonium chloride with ion associates of bromocresol green - quinine and bromophenol blue - quinine in dichlormethane
-
An excess concentration of base quinine (Q) reacts with a sulphonphthalein diacidic dye XH2, (bromocresol green, BCGH2, or bromophenol blue, BPBH2) in dichlormethane solution to form an ion associate (X(2-)(QH21+)2) of stoichiometry 1:2 (dye:amine).Benzethonium chloride (CIB) reacts with the 1:2 ion associate to form an ion associate (QH1+,X2-,B1+) and quinine hydrochloride ClQH(1+).This substitution reaction is a chemical equilibrium with formation constants of 1.50+/-0.67, 1.64+/-0.54, 1.07+/-0.29, 1.04+/-0.20, and 0.84+/-0.26 for BCG and 1.86+/-0.59, 1.47+/-0.23, 1.40+/-0.65, 1.13+/-0.37, and 1.11+/-0.27 for BPB at 283.16, 288.16, 293.16, 298.16, and 303.16 K respectively.The thermodynamic parameters determined by van't Hoff's equation are ΔH0 = -21.766+/-7.482 kJmol-1, ΔS0 = -73+/-51 Jmol-1K-1, and ΔG0 = -1.134+/-0.972 kJmol-1 for BCG and ΔH0 = -18.678+/-7.482 kJmol-1, ΔS0 = -61+/-26 Jmol-1K-1, ΔG0 = -0.916+/-0.401 kJmol-1 for BPB (ΔG0 at 293.16K; and ΔH0 and ΔS0 determined in the range 283-303K). Key words: bromocresol green-quinine-benzetonium, ion associate mixture, bromophenol blue-quinine-benzethonium, equilibrium constants, thermodynamic parameters.
- Gainza, Alberto Hernandez,Konyeaso, Roy Ikemefula
-
p. 937 - 944
(2007/10/02)
-
- Fungicidal and bactericidal method
-
A fungicidal and bactericidal method of imparting fungicidal and bactericidal properties to an article by coating or impregnating the article with a solution of a quaternary ammonium salt of alginic acid or carboxymethyl cellulose (which is insoluble or sparingly soluble in water) in an organic solvent and thereafter removing the solvent from the article.
- -
-
-
