Abstract: Modified amino acid compounds useful for the delivery of active agents are provided. The amino acids, non-alpha-amino acids, have been modified by acylation on the amino group particularly with phenyl or cyclohexyl groups. These groups have a variety of substituents including but not limited to hydroxy, methyl, fluoro, chloro, and the like. The compounds of the invention can be combined with numerous active agents including but not limited to heparin, peptides, and parathyroid hormone, and can then be used for effective administration of the active agent. Administration can be, for example, oral or parenteral.

Abstract: Modified amino acid compounds useful in the delivery of active agents are provided. Methods of administration and preparation are provided as well.

Abstract: The present invention relates to an oral delivery system, and in particular to modified amino acids or peptides for use as a delivery system of sensitive agents such as bioactive peptides. The modified amino acids or peptides can form non-covalent mixtures or microspheres with active biological agents. These mixtures or microspheres are suitable for oral administration of biologically active agents to animals. Methods for the preparation of such amino acids and peptides are also disclosed.

Abstract: Quaternized tertiary aminomethyl acrylamide polymer emulsions are treated by 1) adjusting the pH to about 3.6 to about 4.8, 2) adding a formaldehyde scavenger, 3) adjusting the water content of the aqueous phase to result in about 10-45 weight percent of quaternized aminomethylated acrylamide polymer and 4) heating the resultant emulsion at from about 40.degree. C. to about 80.degree. C. for about 3 to about 20 hours so as to render them more stable, capable of inversion in water independent of water temperature or pH of the medium flocculant and superior dewatering ability.

Abstract: The present invention relates to a delivery system, and in particular to carboxylic acids for use as a delivery system of sensitive agents such as bioactive peptides. The carboxylic acids and salts can form non-covalent mixtures with biologically-active agents. These mixtures are suitable for oral administration of biologically active agents to animals.

Abstract: Polyimides with elevated Tg's are made by imidization of the product of reaction of dianhydrides with diaminobenzotrifluoride and bis(trifluoromethyl) oxydianilines when glass, boron, boron oxides, aluminum oxides or mixtures thereof are incorporated therein.

Abstract: Polymides are made by imidization of the product of reaction of dianhydrides with diaminobenzotrifluoride and bis(trifluoromethyl) oxydianilines. In preferred embodiments the polyimides are end capped with monoanhydride or monoamine residues.

Abstract: Polyimides are made by imidization of the product of reaction of dianhydrides with diaminobenzotrifluoride and bis(trifluoromethyl) oxydianilines. In preferred embodiments the polyimides are end capped with monoanhydride or monoamine residues.

Abstract: Allylic 1-hydroxy alcohols are inverted to allylic 3-hydroxy alcohols by: (1) epoxidizing the allyl group of the allylic 1-hydroxy alcohol to the corresponding 2,3-epoxy-1-hydroxy alcohol; (2) transforming the 2,3-epoxy-1-hydroxy alcohol compound to a 1,2-dihalo-3-hydroxy alcohol; and (3) dehalogenating the 1,2-dihalo-3-hydroxy alcohol to form the desired allylic 3-hydroxy alcohol.

Abstract: A process for chlorinating compounds containing a carbon atom bonded to a hetero-atom selected from the group consisting of oxygen, nitrogen and sulfur; said process comprises contacting the carbon hetero-atom containing compound with a chloro phosphorus complex of the formulaRP.sup..sym. CL.sub.3 P.sup..crclbar. Cl.sub.6wherein R is selected from the group consisting of aryl, substituted aryl, alkyl and substituted alkyl, so that the hetero-atom is replaced by at least one chlorine atom; compounds capable of being chlorinated can include, for example, carboxylic acids, acid chlorides, ketones, aldehydes, alcohols, epoxides, esters, anhydrides, ethers, thiols, and aromatic nitro groups; the reaction can be extended to compounds containing the carbon to chlorine bond alpha to a carbon atom containing at least one hydrogen atom, it can be further dehydrochlorinated, e.g., by either heating to a temperature ranging from about 50.degree. C. to about 300.degree. C. or by reaction with a base selected, e.g.

Abstract: N-succinimidyl haloacetyl aminobenzoates are formed by: (a) reacting an aminobenzoic acid with haloacetylhalide to form a haloacetylaminobenzoic acid; (b) optionally converting the haloacetylaminobenzoic acid from (a) to the ultimately desired halo intermediate compound; (c) reacting the compound from (b) with oxalyl halide to form the corresponding benzoyl compound; and (d) coupling the benzoyl compound from (c) with an N-hydroxysuccinimide to form the ultimately desired N-succinimidyl haloacetyl aminobenzoate.

Abstract: A process for selectively substituting an aromatic nitro group of a nitrophthalic anhydride with a halo group which comprises contacting the nitroaromatic-containing compound with a phosphorus halide of formula:R.sub.n PX.sub.5-nwherein n is selected from 0, 1, 2 and 3; R is selected from the group consisting of C-6 to C-10 aryl and substituted aryl wherein the substituents are selected from the group consisting of: straight and branched chain alkyl, alkoxy, and haloalkyl; halogen, sulfonate and mixtures thereof; and X is a halogen. The process can take place in the presence of an arylphosphorusoxydihalide solvent or without using a solvent. The use of an arylphosphorustetrahalide and particularly phenylphosphorustetrachloride is preferred. The arylphosphorustetrahalide can be prepared in situ by contacting a solution of the corresponding arylphosphorusdihalide in an arylphosphorusoxydihalide solvent with a halogen.

Abstract: The etching of cured arylsiloxane/silicate resin coatings with HF is improved if the curing of said coatings, prior to etching, comprises curing with energy ray irradiation.

Abstract: A process for converting organic hydroxyl-containing compounds to halides which comprises reacting the hydroxyl-containing compound with a phosphorushalide reagent of formula: R.sub.n PX.sub.5-n wherein n is selected from 1, 2 and 3; R is selected from the group consisting of C-6 to C-10 aryl and substituted aryl wherein the substituents are selected from the group consisting of straight and branched chain alkyl, alkoxy, and haloalkyl, halogen, sulfonate and mixtures thereof; and X is a halogen. It is preferred to carry out the reaction in the presence of an arylphosphorusoxydihalide solvent. The use of an arylphosphorustetrahalide and particularly phenylphosphorustetrachloride is preferred. The arylphoshorustetrahalide can be prepared in situ by contacting a solution of the corresponding arylphosphorusdihalide in an arylphosphorusoxydihalide solvent with a halogen. The process can further comprise the step of heating the reaction mixture. Maintaining a reaction temperature of from about 0.degree. C.

Abstract: A process for selectively substituting an aromatic nitro group with a halo group which comprises contacting the nitroaromatic compound with a phosphorushalide of formula: R.sub.n PX.sub.5-n wherein n is selected from 0, 1, 2 and 3; R is selected from the group consisting of C-6 to C-10 aryl and substituted aryl wherein the substituents are selected from the group consisting of: straight and branched chain alkyl, alkoxy, and haloalkyl; halogen, sulfonate and mixtures thereof; and X is a halogen in the presence of an arylphosphorusoxydihalide solvent. The use of an arylphosphorustetrahalide and particularly phenylphosphorustetrachloride is preferred. The arylphosphorustetrahalide can be prepared in situ by contacting a solution of the corresponding arylphosphorusdihalide in an arylphosphorusoxydihalide solvent with a halogen. The process can further comprise the step of heating the reaction mixture to maintain a temperature of from about 100.degree. C. to about 175.degree. C.

Abstract: Liquid para-toluenesulfonyl chloride is reacted with chlorine gas at elevated temperatures in the presence of a catalytic amount of a Lewis acid catalyst, preferably antimony trichloride. Sulfuric acid is added then the reaction mixture is heated and subsequently cooled to about room temperature. Ammonium hydroxide is added then the reaction mixture is distilled to yield a substantially pure 2,6-dichlorotoluene.

Abstract: Novel processes are disclosed for selectively preparing a mixture of certain asymmetric imidazole derivatives and their corresponding regioisomers. The process involves reacting a tautomeric mixture of two precursor compounds with a critical base in the presence of a critical solvent, prior to the desired N-substitution reaction. In general, the base is a hydride of an alkali metal or an alkaline earth metal, or mixtures thereof. Sodium hydride is particularly suitable. The solvents are all non-polar.

Abstract: A method for the dehydroxylation of alpha-hydroxyketone using lithium diphenylphosphide. The alpha-hydroxyketone, e.g. benzoin, is reacted with a solution of lithium diphenylphosphide followed by the addition of either an alkyl halide, e.g. methyliodide, or an alkyl halide and an organic acid, e.g. acetic acid, to yield the dehydroxylated compound, e.g. desoxybenzoin.

Abstract: An improved process is disclosed for preparing racemic 1,1-diphenyl-2-carboethoxycyclopropane from 1,1-diphenylethylene and ethyl diazoacetate as reactants. It involves conducting the reaction in the absence of a metallic-based catalyst and at a reaction temperature sufficiently in excess of 60.degree. C. to permit a yield of at least 20 percent to be obtained. Preferred conditions are given for obtaining yields in excess of 80 percent.Related processes are also disclosed based on certain substituted 1,1-diphenylethylenes with at least one substituent in at least one phenyl group.

Abstract: A compound having the structural formula ##STR1## wherein X is hydrogen or bromine; Y is bromine, phenyl, C.sub.1 -C.sub.4 alkyl or C.sub.4 -C.sub.6 cycloalkyl; R.sup.1 and R.sup.2 independently are C.sub.1 -C.sub.6 alkyl or R.sup.1 and R.sup.2 together form a ring with the nitrogen to which they are attached having 3-8 carbon atoms, optionally substituted with one or two methyl groups.