40137-22-2Relevant articles and documents
PROCESS FOR THE HYDROLYSIS OR ALCOHOLYSIS OF CYCLIC KETAL OR ACETAL GROUPS WITH CARBON DIOXIDE OR AN ALCOHOL
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Page/Page column 7; 8, (2019/02/13)
Process for the hydrolysis or alcoholysis of a ketal or acetal compound wherein a ketal or acetal compound comprising at least one ketal or acetal group and at least one amino group is reacted with carbon dioxide and water oran alcohol.
A high-purity 3 - methylamino - 1, 2 - propylene glycol green synthetic method
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Paragraph 0186-0200, (2017/10/14)
The invention provides a green synthetic method of high-purity 3-methylamino-1,2-propandiol. The method comprises the steps of preparation of glycidol and synthesis of 3-methylamino-1,2-propandiol, wherein the preparation of the glycidol comprises the steps of adding chloro-glycerin and sodium methoxide in methanol, reacting and distilling, and the synthesis of the 3-methylamino-1,2-propandiol comprises the steps of testing pressure, charging, performing amination, recycling monomethylamine and distilling. The green synthetic method has the beneficial effects that the purity of a product prepared by using the green synthetic method is high, the impurity and moisture contents are reduced, the product is colorless transparent sticky liquid in appearance, the purity of the product is 99.87 to 99.96%, and the yield is 98.52 to 98.99%; the yield of the glycidol is 92.61 to 93.76%, and the purity is 99.25 to 99.40%; the production cycle is shortened; the effects of safety and environmental friendliness are achieved; secondary reaction such as polymerization and the like almost does not occur; the effects of energy conservation and consumption reduction are obvious.
PROCESS FOR THE PRODUCTION OF AMINO ALCOHOLS
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Page/Page column 8, (2012/08/28)
The present invention relates to a process for the manufacture of APD and N-alkyl-APD wherein 1-CPD is reacted with aqueous ammonium or aqueous alkyl-amine under alkaline conditions and where the process is conducted in a continuous manner in a reactor comprising a tubular reactor wherein at least two reaction zones are established.
Synthesis Method of 3-Methylamino-1, 2-Propanediol
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Page/Page column 3-4, (2012/11/08)
A synthesis method of 3-methylamino-1,2-propanediol is disclosed in the invention, and it includes the following steps: (1) adding glycerin chlorohydrin, aqueous monomethylamine solution and an amination catalyst, namely NaOH solution and NaHCO3, into a reactor, mixing the material sufficiently, and allowing amination reaction to proceed in two temperature stages; (2) removing monomethylamine and water from the amination solution after the amination reaction is completed, filtering out the solid resultant, and feeding the filtrate into a still; (3) distilling under reduced pressure to obtain 3-methylamino-1,2-propanediol, wherein the vacuum for distillation under reduced pressure is equal to or greater than 0.099 MPa and the temperature is 130-160° C. The product synthesized according to the invention, a liquid appearing colorless and transparent, has increased purity of over 99.5% (GC) and decreased impurities. Therefore, when this product is used for synthesis of iopromide as a hypo-osmolar nonionic contrast medium, it exactly meets the quality demand.
A process for the prepration of a dihydroxyamino compound
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Page 17-20, (2008/06/13)
Disclosed are a process for the preparation of a dihydroxyamino compound in which water and discoloring ingredients are removed while preventing decomposition of a dihydroxyamino compound by distilling a crude reaction liquid containing an epoxy compound and an amino compound at a specified temperature and pressure, a process for improving a yield of a dihydroxyamino compound having high purity by recirculating an aqueous solution of an amino compound recollected from a crude reaction liquid into a reaction step, and a process in which there are prevented discoloration and a yield decline of a dihydroxyamino compound.
PEPTIDE NUCLEIC ACID CONJUGATES
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, (2008/06/13)
A novel class of peptide nucleic acids are described which include a conjugate attached thereto. The peptide nucleic acids generally comprise ligands such as naturally occurring DNA bases attached to a peptide backbone through a suitable linker.
Process for the preparation of a dihydroxyamino compound
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, (2008/06/13)
Disclosed are a process for the preparation of a dihydroxyamino compound in which water and discoloring ingredients are removed while preventing decomposition of a dihydroxyamino compound by distilling a crude reaction liquid containing an epoxy compound and an amino compound at a specified temperature and pressure, a process for improving a yield of a dihydroxyamino compound having high purity by recirculating an aqueous solution of an amino compound recollected from a crude reaction liquid into a reaction step, and a process in which there are prevented discoloration and a yield decline of a dihydroxyamino compound.
Synthesis and Hydrolytic Lability of α-Phenoxyacetamides Containing Hydroxy Groups in the N-alkyl Residue
Anelli, Pier Lucio,Brocchetta, Marino,Canipari, Sonia,Losi, Pietro,Manfredi, Giuseppe,et al.
, p. 135 - 142 (2007/10/03)
Secondary and tertiary amides of 3,5-biscarbonyl>phenoxyacetic acid bearing hydroxy groups in positions β (β-OH) and γ (γ-OH) relative to the acetamide nitrogen atom have been synthesized.Such amides easily undergo cleavage of the acetamide bond in water at neutral pH.Hydrolysis rate constant for a series of such amides and protonation constants for the corresponding leaving amines were determined.No simple correlation between the two parameters could be found.A study of the dependence of these parameters on the structural features of the substrates, such as the presence of an N-methyl group and number of β-OH and γ-OH groups, was carried out.All these features lead to enhancement of the amide hydrolysis rate and a synergistic effect is operative when both N-methyl and β-OH groups are contained in the substrate.Presence of a methyl group increases the basicity of amines whereas β-OH and γ-OH groups have the opposite effect.Mechanistic speculations seem to indicate that the abnormal lability of the acetamide bond is due to protic-like catalysis by an intramolecular OH...N hydrogen bond.
Tyrosine kinase inhibitors. 13. Structure - Activity relationships for soluble 7-substituted 4-[(3-bromophenyl)amino]pyrido[4,3-d]pyrimidines designed as inhibitors of the tyrosine kinase activity of the epidermal growth factor receptor
Thompson, Andrew M.,Murray, Donna K.,Elliott, William L.,Fry, David W.,Nelson, James A.,Showalter, H.D. Hollis,Roberts, Bill J.,Vincent, Patrick W.,Denny, William A.
, p. 3915 - 3925 (2007/10/03)
The general class of 4-(phenylamino)quinazolines are potent (some members with IC50 values 40 mM) and retention of overall inhibitory activity (IC50's of 0.5-10 nM against isolated enzyme and 8-40 nM for inhibition of EGFR autophosphorylation in A431 cells) were weakly basic amine derivatives. These results are broadly consistent with a proposed model for the binding of these compounds to EGFR, in which the 6- and 7-positions of the pyridopyrimidine ring are in a largely hydrophobic binding region of considerable steric freedom, at the entrance of the adenine binding cleft. The most active cationic analogues have a weakly basic side chain where the amine moiety is three or more carbon atoms away from the nucleus. Two of the compounds (bearing weakly basic morpholinopropyl and strongly basic (dimethylamino)butyl solubilizing groups) produced in vivo tumor growth delays of 13-21 days against advanced stage A431 epidermoid xenografts in nude mice, when administered ip twice per day on days 7-21 posttumor implant. Treated tumors did not increase in size during therapy and resumed growth at the termination of therapy, indicating an apparent cytostatic effect for these compounds under these treatment conditions. The data suggest that continuous long-term therapy with these compounds may result in substantial tumor growth inhibition.
The reaction of sulfamic acid derivatives with epoxides. 4. Hydrolysis of 3-chloro-2-hydroxypropylsulfamates
Tartakovsky,Ermakov,Mal'chevsky,Kulikova
, p. 2667 - 2668 (2007/10/03)
Under basic hydrolysis conditions 3-chloro-2-hydroxypropylsulfamates transform into 2,3-dihydroxypropylsulfamates. Acidic hydrolysis of the latter leads to 3-alkylaminopropane-1,2-diols.
