Patent classifications
C07C231/02
Use of ruthenium complexes for preparing amides, polypeptides and cyclic dipeptides
A process for preparing amides by reacting a primary amine and a primary alcohol in the presence of a Ruthenium complex to generate the amide and molecular hydrogen. Primary amines are directly acylated by equimolar amounts of alcohols to produce amides and molecular hydrogen (the only byproduct) in high yields and high turnover numbers. Also disclosed are processes for hydrogenation of amides to alcohols and amines; hydrogenation of organic carbonates to alcohols; hydrogenation of carbamates or urea derivatives to alcohols and amines; amidation of esters; acylation of alcohols using esters; coupling of alcohols with water and a base to form carboxylic acids; dehydrogenation of beta-amino alcohols to form pyrazines and cyclic dipeptides; and dehydrogenation of secondary alcohols to ketones. These reactions are catalyzed by a Ruthenium complex which is based on a dearomatized PNN-type ligand of formula A1 or precursors thereof of formulae A2 or A3.
Processes and intermediates for making sweet taste enhancers
The present invention includes methods/processes and intermediates for preparing compounds having structural Formula (I): ##STR00001##
wherein X is alkyl, substituted alkyl, alkenyl, substituted alkenyl, heteroalkyl, substituted heteroalkyl, heteroalkenyl, or substituted heteroalkenyl.
Processes and intermediates for making sweet taste enhancers
The present invention includes methods/processes and intermediates for preparing compounds having structural Formula (I): ##STR00001##
wherein X is alkyl, substituted alkyl, alkenyl, substituted alkenyl, heteroalkyl, substituted heteroalkyl, heteroalkenyl, or substituted heteroalkenyl.
Polyamine transport inhibitors as novel therapeutics
Novel polyamine transport inhibitors have been synthesized and demonstrated to block the uptake of native polyamines into human cancer cells. A combination therapy of the transport inhibitor and DFMO (a drug which blocks polyamine biosynthesis) provided synergistic activity against a metastatic human colon cancer cell line. The strategy uses polyamine depletion and polyamine metabolism to generate reactive oxygen species within cells as a novel way to treat cancers. This approach may be implemented for widespread use in the treatment of diseases which rely upon polyamine transport activity for proliferation.
Polyamine transport inhibitors as novel therapeutics
Novel polyamine transport inhibitors have been synthesized and demonstrated to block the uptake of native polyamines into human cancer cells. A combination therapy of the transport inhibitor and DFMO (a drug which blocks polyamine biosynthesis) provided synergistic activity against a metastatic human colon cancer cell line. The strategy uses polyamine depletion and polyamine metabolism to generate reactive oxygen species within cells as a novel way to treat cancers. This approach may be implemented for widespread use in the treatment of diseases which rely upon polyamine transport activity for proliferation.
PREPARATION OF CATIONIC SURFACTANTS
Compositions that include cationic surfactants and methods of synthesizing compositions that include cationic surfactants. The surfactants include a quaternary amine and a saturated or unsaturated alkyl chain with 4 to 28 carbons. The surfactants can be generated by reacting a fatty acid modified with an amino alkyl group and an epihalohydrin in the presence of a base. The cationic surfactants can be generated by reacting a fatty acid modified with an amino alkyl group, an epihalohydrin, and a carboxylic acid. The cationic surfactants can be generated by reacting a carboxylic acid, an epihalohydrin, and a catalyst to afford a halo-substituted alkyl ester, followed by reacting the halo-substituted alky ester with a fatty acid modified with an amino alkyl group.
PREPARATION OF CATIONIC SURFACTANTS
Compositions that include cationic surfactants and methods of synthesizing compositions that include cationic surfactants. The surfactants include a quaternary amine and a saturated or unsaturated alkyl chain with 4 to 28 carbons. The surfactants can be generated by reacting a fatty acid modified with an amino alkyl group and an epihalohydrin in the presence of a base. The cationic surfactants can be generated by reacting a fatty acid modified with an amino alkyl group, an epihalohydrin, and a carboxylic acid. The cationic surfactants can be generated by reacting a carboxylic acid, an epihalohydrin, and a catalyst to afford a halo-substituted alkyl ester, followed by reacting the halo-substituted alky ester with a fatty acid modified with an amino alkyl group.
PROCESS FOR PREPARING ESTERS OF N-ACYLATED AMINO ACIDS WITH ACID-LABILE KETO PROTECTIVE GROUP FUNCTIONS
The present invention relates to a novel process for the esterification of N-acylated amino acids which contain an acid-labile keto protective group under alkaline conditions without using a polar aprotic solvent, in which the N-acylated amino acid with acid-labile keto protective group prepared in situ is esterified using an alkyl halide or a mono- or dialkyl ester of sulfuric acid.
VOLTAGE GATED SODIUM CHANNEL IMAGING AGENTS
Provided herein are radiolabeled compounds useful for minimally invasive imaging techniques. An exemplary radiolabeled compound provided herein is useful as a radiotracer for position emission tomography imaging of voltage gated sodium channels. Methods for prepared unlabeled and labeled compounds, and diagnostic methods using the compounds are also provided.
Process method for producing pesticide by using carbon dioxide
A process method for producing a pesticide by using carbon dioxide includes: weighing a 1,3-cyclohexanedione substrate 1(a-e), a catalyst and Cs.sub.2CO.sub.3 in a Schlenk bottle, degassing, and continuously introducing 1 atm of carbon dioxide; adding a solvent and reacting for 48 h in an oil bath at 50° C. After the reaction was completed, post-treatment was carried out to obtain a 2-carboxyl-1,3-cyclohexanedione compound 2(a-e). The obtained acid is acylated and then added dropwise to a dichloromethane solution containing aniline to react for 2 h at room temperature. After the reaction, column chromatography was performed to obtain a pesticide compound 3(a-e). Adding the pesticide compound 3(a-e) into 50% concentrated sulfuric acid and refluxing at 80° C. for 8 hours. Through separation, a pesticide product compound 4(a-e) was obtained. The process method is simple, with low requirements on equipment, wide sources of raw materials, low cost, low toxicity and easy industrial scale-up production.