专利号:US-5939304-A 优先权日:1997-06-05 标题:Method for synthesis of anhydrothrombin 发明人:SUZUKI TOYOAKI; HOSOKAWA KAZUYA; NAGATA MASANORI 权利人:FUJIMORI KOGYO CO 摘要:A method for a synthesis of anhydrothrombin is provided which features a short process, an easy procedure, and high yields. n The method comprises n (A) a step of causing an active serine residue site of thrombin to react with an inhibitor, n (B) a step of performing an alkali treatment at a pH of not less than 11, and n (C) a step of performing an operation of recovery, and carries out these steps sequentially in the order mentioned, and is characterized by causing at least the step of performing the operation of recovery to proceed in the presence of at least one compound selected from the group consisting of polyhydric alcohols and saccharides, and a salt or an amphoteric electrolyte.
专利号:WO-2021023634-A1 优先权日:2019-08-05 标 题 :PROCESS FOR THE SYNTHESIS OF PITOLISANT HCl 发明人:COLOMBANO GIAMPIERO; BARBERO MAURO; BOGOGNA LUIGI; ROLETTO JACOPO; PAISSONI PAOLO 权利人:PROCOS SPA 摘要:Disclosed is a process for the synthesis of pitolisant HCl of formula (I), from piperidine and 1-bromo-3-chloropropane. The process according to the invention is economically efficient and easily industrially scalable.
专利号:US-2022098170-A1 优先权日:2019-01-16 标 题 :Process for the synthesis of gepirone 发明人:COLOMBANO GIAMPIERO; BARBERO MAURO; GIOVENZANA GIOVANNI BATTISTA; ROLETTO JACOPO; PAISSONI PAOLO 权利人:PROCOS SPA 摘要:Disclosed is a process for the synthesis of gepirone of formula (I) from 8-(pyrimidin-2-yl)-5,8-diazaspiro[4,5]decan-5-ium bromide. The process according to the invention is economically efficient and easily industrially scalable.
专利号:US-9024030-B2 优先权日:2012-01-13 标题 :Process for the synthesis of etoricoxib 发明人:MAO ZHENMIN; LAN TIAN; LIU LANFANG; YAN LONG; BECKER STEFAN 权利人:TIEFENBACHER ALFRED E GMBH & CO KG; SHANGHAI GOLDEN PHARMATECH CO LTD; SHANGHAI GOLDEN PHARMATECH CO LTD 摘要:The present invention relates to a process for the synthesis of the anti-inflammatory agent 5-chloro-3-(4-methanesulfonylphenyl)-6′-methyl-[2,3′]bipyridine, referred to as compound of formula (1) or etoricoxib, which is a pharmaceutically active ingredient inhibiting cyclooxygenase-2. In particular, the application concerns a novel process of making the compound of formula (1) by oxidizing a compound of formula (4).
专利号:US-6939962-B2 优先权日:2000-07-31 标题:Method for the synthesis of sucrose-6-esters 发明人:CLARK JASON D; LEMAY JR RICHARD R 权利人:TATE & LYLE PLC 摘要:There is described a process for the synthesis of a sucrose-6-ester comprising: (a) reacting a mixture comprising sucrose and a polar aprotic solvent with an organotin-based acylation promoter, while adding a solvent capable of removing water by co-distillation, and removing water by co-distillation, to afford a first reaction mixture which is substantially free from water, followed by (b) adding a carboxylic anhydride to said first reaction mixture to afford a second reaction mixture, and maintaining said second reaction mixture at a temperature and for a period of time sufficient to produce a sucrose-6-ester, characterised in that step (a) is performed at a temperature of from 85 to 125° C. and at a pressure of from 20 to 80 kPa. In the most preferred embodiment, the polar aprotic solvent is DMF, the solvent capable of removing water by co-distillation is cyclohexane, the organotion-based acylation promoter is a 1,3-diacyloxy-1,1,3,3-tetrabutyldistannoxane, and step (a) is performed at approximately 97° C., and approximately 50 kpa, until the weight ratio of tin to water in the first reaction mixture is greater than about 26, when the tin content is measured by X-Ray Fluoresence Analyzer, and the water content is measured by the Karl-Fischer method.
专利号:US-11713329-B2 优先权日:2018-12-10 标 题 :Intermediates useful in the preparation of halichondrin compounds and methods for preparing the same 发明人:XU WEIPING 权利人:BEIJING TIENYI LUFU PHARMATECH CO LTD 摘要:The invention relates to intermediates useful in the preparation of halichondrin compounds, methods for preparing the same and use thereof, such as halichondrins, eribulin, or their analogs. The intermediates, the methods and use thereof are used for the synthesis of the C20-C26 fragment of halichondrin compounds. The raw materials in the synthetic route of the invention are cheap and easily obtained, the sources and the qualities of the raw materials are reliable. The choice of the methods useful in the synthesis of chiral central structures are based on the structural characteristics of the reactants, thus effectively improving the synthesis efficiency, reducing the difficulties and risks of product quality control, and avoiding the use of highly toxic and expensive organotin catalysts to significantly decrease costs and improve environmental friendliness.