专利号:US-2025313590-A1 优先权日:2024-03-16 标题:Phosphoramidite morpholino monomers towards synthesis/convergent synthesis of PMO, TMO, their chimera oligos in 5 prime to 3 prime direction 发明人:SINHA SURAJIT; GHOSH ATANU; BANERJEE ARPAN 权利人:INDIAN ASS FOR THE CULTIVATION OF SCIENCE 摘要:The present invention relates to 5′-morpholino amidite monomers as 5′-CE/5′- t Bu phosphoramidite morpholino monomers (2) and process chemistry for the efficient synthesis of N-Trityl or monomethoxytrityl (MMTr)-protected 5′-morpholino amidite monomers and their use in the synthesis of phosphorodiamidate morpholino oligonucleotides (PMO), thiophosphoramidate morpholino oligonucleotides (TMO) and their chimeras which can be used for antisense technology or in general oligonucleotides related research.
专利号:WO-2021014395-A1 优先权日:2019-07-24 标题:Process for the synthesis of deuterated capsaicin, capsaicinoids and synthetic capsaicin analogs 发明人:ORUGANTI SRINIVAS; AMRUTAPU SRAVANTH KUMAR; SAMPATH MAGESH; SEN SAIKAT 权利人:DR REDDY’S INST OF LIFE SCIENCES 摘要:The present application provides novel processes for the synthesis of deuterated intermediates of capsaicinoids, particularly II, III, IV and V of capsaicinoids, relating to pharmaceutical applications. The invention also provides novel intermediates of compounds of formula IX, XIV, XV, XVI, XVII, XVIII, XX and XXI utilized in the process of making deuterated capsaicin II, III, IV and V.
专利号:EP-4092127-A1 优先权日:2021-05-18 标题:Enzyme-catalytic method for the direct stereoselective synthesis of gamma-(acyloxy) carboxylic acids 发明人:PARVE JAAN; KUDRJASHOVA MARINA; GATHERGOOD NICHOLAS; PARVE OMAR 权利人:TALLINN UNIV OF TECHNOLOGY 摘要:The present invention is a method for the stereoselective straightforward synthesis of gamma-acyloxy carboxylic acids of novel structure starting from racemic gamma-hydroxy carboxylic acid salts that are obtained by alkaline hydrolysis of the racemic gamma-lactones. The salt is acylated by enzyme catalysis in an organic solvent containing an acyl donor and an immobilised lipase, on stirring at room temperature (ca 20 °C) until reaching the conversion rate required. After that, the reaction mixture is acidified and extracted and the product treated with catalytic amount of para-toluenesulfonic acid in toluene during the time required for the relactonisation of the unreacted salt enantiomer. Thereafter, the target gamma-acyloxy carboxylic acid formed from one enantiomer of the starting compound and relactonised gamma-lactone formed from the other, unreacted enantiomer of the starting compound are isolated using a routine separation method, such as distillation, extraction with NaHCO3 water solution followed by acidification or column chromatography.
专利号:US-2024409495-A1 优先权日:2021-10-20 标 题 :Process for the preparation of 2,7-dihydroxy-9-fluorenone useful for the synthesis of tilorone and its salts 发明人:JAISANKAR PARASURAMAN; DEB INDUBHUSAN; BHATTACHARJEE PINAKI 权利人:COUNCIL SCIENT IND RES 摘要:Methods involving preparation of building blocks of 2,7-dihydroxy-9-fluorenone toward the synthesis of tilorone dihydrochloride salt and other salts (bromide, iodide, fluoride, citrate, oxalate, maleate, phosphate, tartrate, triflate, trifluoroacetate, tetrafluoroborate) of tilorone, and an efficient, safe, cost effective method for the preparation of 2,7-bis-[2-(diethylamino)ethoxy]-fluorenone-9 and its various salts are developed. The methods involve oxygenation of fluorene, nitration of fluorenone, followed by reduction and diazotization toward the formation of 2,7-dihydroxy-9-fluorenone, which is the key intermediate for the formation of 2,7-bis-[2-(diethylamino)ethoxy]-9-fluorenone-dihydrochloride (Tilorone dihydrochloride) and other tilorone salts. The synthesis method has relatively simple operation, mild reaction conditions, high yield, and simple process with yields of 80-97%. Subsequent product purification of this method uses filtration and crystallization methods, avoiding the existing methods of column chromatography. Therefore, the research of its synthetic method being with a wide range of applications from the drug development and material synthesis point of view.
专利号:US-8350031-B2 优先权日:2008-06-02 标 题:Processes for the synthesis of levocetirizine and intermediates for use therein 发明人:RAO DHARMARAJ RAMACHANDRA; KANKAN RAJENDRA NARAYANRAO; GHAGARE MARUTI; CHIKHALIKAR SANDIP VASANT 权利人:CIPLA LTD; RAO DHARMARAJ RAMACHANDRA; KANKAN RAJENDRA NARAYANRAO; GHAGARE MARUTI; CHIKHALIKAR SANDIP VASANT 摘要:The present invention provides a compound of formula (IV) n nwherein R is Cl, Br, NO 2 , OH or OR′, and R′ is alkyl, and its use in the synthesis of levocetirizine, including its use in the synthesis of (−)-1-[(4-chlorophenyl)-phenylmethyl]piperazine, an intermediate useful in the synthesis of levocetirizine. The present invention also provides compounds (II) and (III) which are useful in the synthesis of compound (IV).
专利号:US-11661406-B2 优先权日:2018-08-13 标 题 :Method for producing intermediate useful for synthesis of SGLT inhibitor 发明人:LI QING RI; YOON HEE KYOON 权利人:DAEWOONG PHARMACEUTICAL CO LTD 摘要:A method of preparing an intermediate useful for the synthesis of a diphenylmethane derivative that can be used as an SGLT inhibitor is described. A method of synthesizing a compound of Formula 7 can address problems of existing synthesis processes requiring the synthesis of the Grignard reagent and management of related substances. In addition, the method can minimize the generation of related substances, and thus does not require reprocessing of reaction products, thereby simplifying the process. Accordingly, the production yield of a diphenylmethane derivative can be maximized.
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