专利号:US-9788548-B2 优先权日:2013-12-13 标题:Synthesis of pure diallyl morpholinium monomers in high yields and using antibacterial effect of their spiro polymers 发明人:BICAK TUGRUL CEM; INCE AHMET; BICAK NIYAZI 权利人:BICAK TUGRUL CEM; Tugrul Cem BICAK 摘要:Herein, the synthesis of N,Ndiallyl morpholinium monomers and polymerization of the same to form rings at high yield and purity are explained. The process involves the synthesis of N,Ndiallyl morpholinium bromide and chloride and subsequently partially or completely exchanging their anions with borate, p-toluenesulfonate, oleate, and acetate anions. The cyclopolimerization of monomers yields water soluble polymers carrying quaternary ammonium groups in each repeated unit, whose aqueous solutions act as a bactericide solution. These solutions are advantageous in preparation of antibacterial formulations intended for domestic use. The polymer with bromide and borate anions is an efficient antibacterial which is able to kill “ Pseudomonas Aeruginosa â€?, the hardest hospital bacterium to cope with, as well as various common bacteria. These formulations are suitable for producing bactericide wet wipes and forming abacterial surfaces and, when combined with air conditioners, generating bacteria free air.
专利号:US-4097479-A 优先权日:1977-03-11 标题 :Synthesis of 5-substituted tetrazoles 发明人:LEIPZIG THEODORE J 权利人:MILES LAB 摘要:Synthesis of 5-substituted tetrazoles via reaction of an organic nitrile with azide anion is improved by performing the reaction in an amine as solvent and in the presence of an acid-addition salt of the amine as catalyst.
专利号:WO-2022153263-A1 优先权日:2021-01-18 标 题 :Process for the synthesis of imepitoin 发明人:VERONESE MARTINO; BAROZZA ALESSANDRO; BETTONI PIERGIORGIO; ROLETTO JACOPO; PAISSONI PAOLO 权利人:PROCOS SPA 摘要:Disclosed is a process for the synthesis of imepitoin of formula (I) by reacting 4- chloroaniline, chloroacetic acid and urea in the presence of an apolar or weakly polar aprotic solvent such as xylene, and then reacting the resulting 1-(4- chlorophenyl)imidazolidine-2, 4-dione (II) with morpholine in the presence of morpholine hydrochloride. Crystallisation from dimethyl sulphoxide and methanol provides pure imepitoin (I). The process is cheaper and more easily industrially scalable than the known procedures, thus enabling imepitoin to be produced with high yields and limited costs.
专利号:US-6172226-B1 优先权日:1993-12-22 标 题:Synthons for the synthesis and deprotection of peptide nucleic acids under mild conditions 发明人:COULL JAMES M; EGHOLM MICHAEL; HODGE RICHARD P; ISMAIL MOHAMED; RAJUR S B 权利人:PERSEPTIVE BIOSYSTEMS INC 摘要:A method is disclosed for preparing novel PNA synthons having protecting groups capable of removal under mild conditions. The PNA synthons are prepared by coupling novel N-substituted nucleobase intermediates having carbamate protection of the exocyclic amino group of the heterocycle to an amino protected backbone or an amino protected backbone ester of the amino acid N-(2-aminoethyl)-glycine. By the method of this invention, the resultant PNA synthons can have orthogonal protection of the carbamate protected nucleobase and the amino protected backbone. The PNA synthons are useful in the synthesis of peptide nucleic acids (PNAs) and other oligomers such as PNA-DNA chimeras, and may be used in automated synthesizers. Novel compositions of matter are also disclosed. In addition, a guanine PNA synthon having selective carbamate protection of the exocyclic 2-amino group with the C6 carbonyl group unprotected is disclosed.
专利号:US-7153960-B2 优先权日:2001-12-10 标 题:Synthesis of 4,5-dihydro-pyrazolo[3,4-c]pyrid-2-ones 发明人:ZHOU JIACHENG; OH LYNETTE M; MA PHILIP; LI HUI-YIN; CONFALONE PASQUALE 权利人:BRISTOL MYERS SQUIBB CO 摘要:A novel process and intermediates thereof for making 4,5-dihydro-pyrazolo[3,4-c]pyrid-2-ones of the type shown below from appropriate phenyl hydrazines is described. n nThese compounds are useful as factor Xa inhibitors.
专利号:WO-2025098683-A1 优先权日:2023-11-10 标 题:Improved process for the synthesis of imepitoin 发明人:ESTEVEZ LORA RAÚL; GARCÃ?A RAMOS Ã?LVARO; MARTINEZ GRAU MARÃ?A Ã?NGELES 权利人:JUSTESA IMAGEN S A U 摘要:The present invention describes an improved process for the preparation of imepitoin by means of an efficient preparation of its intermediate 1-(4- chlorophenyl)imidazolidine-2,4-dione followed by condensation with morpholine in the presence of ammonium chloride. Particularly, the invention relates to a process which provides imepitoin in high yield by removing the water generated in the reaction using a continuous process to distil, dry and recirculate the dried morpholine back to the reactor. More particularly, the invention relates to a process that provides imepitoin with very high purity by a simple washing with toluene and water. Still more particularly, the invention relates to a cost-effective process that is scalable for industrial application.