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:US-9763452-B2 优先权日:2012-06-11 标 题 :Synthesis of MOFs 发明人:MORRIS RUSSELL EDWARD; WHEATLEY PAUL STEWART; WARRENDER STEWART; DUNCAN MORVEN 权利人:UNIV COURT UNIV ST ANDREWS; UNIVERISTY COURT OF THE UNIV OF ST ANDREWS 摘要:The present invention relates to the synthesis of a variety of metal organic frameworks (MOFs) using low temperature and solvents which are considered to be not particularly harmful to the environment. There is also provided novel MOFs which may be made by the desired processes.
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:WO-2025053792-A1 优先权日:2023-09-06 标题:Collective synthesis of phantomolin family through total synthesis of the sesquiterpene lactone molephantin 发明人:CHIBA SHUNSUKE; PATOURET REMI HENRI LOUIS; LI HOI YEUNG; LAI SOAK KUAN 权利人:UNIV NANYANG TECH 摘要:Disclosed herein are processes to generate an intermediate in the total synthesis of (+)- molephantin or a derivative thereof, and a total synthesis of (+)-molephantin or a derivative thereof. Also disclosed herein are methods of forming a compound of formula XIV and of forming a compound of formula XV, wherein compound of formula XIV and compound of formula XV are as defined in the description.
专利号:US-8436206-B2 优先权日:2007-08-03 标 题:Process for the synthesis of (7-methoxy-1-naphthyl) acetonitrile and application in the synthesis of agomelatine 发明人:DUBUFFET THIERRY; LECOUVE JEAN-PIERRE; HERMET JEAN-PAUL 权利人:DUBUFFET THIERRY; LECOUVE JEAN-PIERRE; HERMET JEAN-PAUL; SERVIER LAB 摘要:Process for the industrial synthesis of the compound of formula (I) n nApplication of such process in the synthesis of agomelatine.
[参考文献]: C F Brayton. Dimethyl Sulfoxide (Dmso): A Review. Cornell Vet. 1986 Jan;76(1):61-90. [参考文献]: William F Rawls, Et Al. Dimethyl Sulfoxide (Dmso) As Intravesical Therapy For Interstitial Cystitis/bladder Pain Syndrome: A Review. Neurourol Urodyn. 2017 Sep;36(7):1677-1684. [参考文献]: Diana S M Ottoz, Et Al. Inducible, Tightly Regulated And Growth Condition-Independent Transcription Factor In Saccharomyces Cerevisiae. Nucleic Acids Res. 2014;42(17):E130. [参考文献]: Elena Peira, Et Al. The Influence Of Surface Charge And Photo-Reactivity On Skin-Permeation Enhancer Property Of Nano-Tio In Ex Vivo Pig Skin Model Under Indoor Light. Int J Pharm. 2014 Jun 5;467(1-2):90-9. [参考文献]: Jin-Ping Li, Et Al. The Investigational Aurora Kinase A Inhibitor Alisertib (Mln8237) Induces Cell Cycle G2/m Arrest, Apoptosis, And Autophagy Via P38 Mapk And Akt/mtor Signaling Pathways In Human Breast Cancer Cells. Drug Des Devel Ther. 2015 Mar 16:9:1627-52.
合成参考文献
参考文献:10.1104/pp.109.148742 摘要:Hosein FN, Bandyopadhyay A, Peer WA, Murphy AS. The catalytic and protein-protein interaction domains are required for APM1 function. Plant Physiol. 2010 Apr;152(4):2158–72. 参考文献:10.1530/rep-09-0549 摘要:Higaki S, Eto Y, Kawakami Y, Yamaha E, Kagawa N, Kuwayama M, Nagano M, Katagiri S, Takahashi Y. Production of fertile zebrafish (Danio rerio) possessing germ cells (gametes) originated from primordial germ cells recovered from vitrified embryos. Reproduction. 2010 Apr;139(4):733–40. doi: 10.1530/rep-09-0549. 参考文献:10.1097/ccm.0b013e3181d44e06 摘要:Chen LW, Tseng HT, Chen PH, Hsu CM. Peritonitis-induced peroxynitrite and lung damage depends on c-Jun NH2-terminal kinase signaling of hematopoietic cells. Crit Care Med. 2010 Apr;38(4):1168–78. doi: 10.1097/ccm.0b013e3181d44e06. 参考文献:10.1007/s10549-010-0765-7 摘要:Di X, Gennings C, Bear HD, Graham LJ, Sheth CM, White KL, Gewirtz DA. Influence of the phosphodiesterase-5 inhibitor, sildenafil, on sensitivity to chemotherapy in breast tumor cells. Breast Cancer Research and Treatment. 2010 Feb 13;124(2):349–60. doi: 10.1007/s10549-010-0765-7. 参考文献:10.1007/s12031-010-9333-1 摘要:Yoon JS, Yang H, Kim SH, Sung SH, Kim YC. Limonoids from Dictamnus dasycarpus Protect Against Glutamate-induced Toxicity in Primary Cultured Rat Cortical Cells. Journal of Molecular Neuroscience. 2010 Feb 13;42(1):9–16. doi: 10.1007/s12031-010-9333-1.