专利号:WO-2024013633-A1 优先权日:2022-07-11 标 题 :Process for the synthesis of vitamin k2 发明人:SHASTRI MAYANK; BAIKAR MRUNALI H; VORA PARIN K; BNS RAJU 权利人:SYNERGIA LIFE SCIENCES PVT LTD 摘要:The present disclosure relates to the synthesis of Vitamin K2 bearing varying prenyl side chains. The synthesis comprises the reaction of phenyl sulfone of tert-butyl dimethyl silyl (TBDMS) protected mono prenyl menadiol with prenyl halides bearing varying prenyl units in the presence of the phase transfer catalyst followed by reductive desulphonation to yield TBDMS ether of Vitamin K2. The TBDMS ether is then oxidized in the presence of chromium trioxide and periodic acid to yield the corresponding Vitamin K2.
专利号:WO-2012047907-A9 优先权日:2010-10-04 标题 :Synthesis of c5-substituted tetracyclines, uses thereof, and intermediates thereto 发明人:MYERS ANDREW G; WRIGHT PETER M; HECKER EVAN 权利人:HARVARD COLLEGE; MYERS ANDREW G; WRIGHT PETER M; HECKER EVAN 摘要:The tetracycline class of antibiotics has played a major role in the treatment of infectious diseases for the past 50 years. However, the increased use of the tetracyclines in human and veterinary medicine has led to resistance among many organisms previously susceptible to tetracycline antibiotics. The recent development of a modular synthesis of tetracycline analogs through a chiral enone intermediate has allowed for the efficient synthesis of novel tetracycline analogs never prepared before. The present invention provides more efficient routes for preparing the enone intermediate and allows for a wide variety of substituents at position 5 of the tetracycline ring system.
专利号:US-9688644-B2 优先权日:2009-04-30 标 题 :Synthesis of Tetracyclines and intermediates thereto 发明人:MYERS ANDREW G; KUMMER DAVID A; LI DERUN; HECKER EVAN; DION AMELIE; WRIGHT PETER M 权利人:HARVARD COLLEGE 摘要:The tetracycline class of antibiotics has played a major role in the treatment of infectious diseases for the past 50 years. However, the increased use of the tetracyclines in human and veterinary medicine has led to resistance among many organisms previously susceptible to tetracycline antibiotics. The recent development of a modular synthesis of tetracycline analogs through a chiral enone intermediate has allowed for the efficient synthesis of novel tetracycline analogs never prepared before. The present invention provides more efficient routes for preparing the enone intermediate and allows for substituents at positions 4a, 5, 5a, and 12a of the tetracycline ring system.
专利号:US-8957230-B2 优先权日:2011-06-30 标 题 :Synthesis of cleistanthin A and derivatives thereof 发明人:MULIK NILESH SHRIDHAR; PANGHAVANE KAILASH DATTATRAYA 权利人:MULIK NILESH SHRIDHAR; PANGHAVANE KAILASH DATTATRAYA 摘要:The present invention provides a method for preparing Cleistanthin A, a diphyllin glycoside, derivatives thereof and intermediates thereto. In particular the present invention provides in one of the aspect a method for synthesis of compound of formula D a key intermediate of diphyllin, which can be carried out in a shorter duration and at an ordinary temperature.
专利号:US-6472534-B2 优先权日:1999-10-21 标 题:Methods for the preparation of intermediates in the synthesis of HIV-protease inhibitors 发明人:BORER BENNETT C; ZOOK SCOTT E; BUSSE JULIETTE K 权利人:AGOURON PHARMA 摘要:Methods for the preparation of chemical intermediates in the synthesis of HIV-protease inhibitors related to and including nelfinavir mesylate are disclosed. The method of this invention comprises converting tetrohydran derivatives into oxazolines to provide key reaction intermediates for the preparation of nelfinavir. Also disclosed is a method for the preparation of a chiral amino alcohol from an epoxy-tetrahydrofuran.
专利号:US-2025171493-A1 优先权日:2022-03-05 标题 :Processes for synthesis of withanolides and withaferins and analogs thereof 发明人:LOPCHUK JUSTIN MATTHEW 权利人:H LEE MOFFITT CANCER CT & RES 摘要:The present disclosure provides processes for the synthesis of withanolides such as Withanolide A and Withanolide D.
[参考文献]: Lee H, Et Al. Genotoxicity Of 1,3-Dithiane And 1,4-Dithiane In The Cho/sce Assay And The Salmonella/microsomal Test. Mutat Res. 1994 Jun;321(4):213-8. [参考文献]: Martinez Ra, Et Al. Synthesis Of Isotopically Labeled 1,3-Dithiane. J Labelled Comp Radiopharm. 2014 May 15;57(5):338-41. [参考文献]: H Lee, Et Al. Genotoxicity Of 1,3-Dithiane And 1,4-Dithiane In The Cho/sce Assay And The Salmonella/microsomal Test. Mutat Res. 1994 Jun;321(4):213-8. [参考文献]: Makoto Michida, Et Al. Lewis Base Catalyzed 1,3-Dithiane Addition To Carbonyl And Imino Compounds Using 2-Trimethylsilyl-1,3-Dithiane. Chem Asian J. 2008 Sep 1;3(8-9):1592-600. [参考文献]: Nasser Iranpoor, Et Al. A New Approach To The Reduction Of Sulfoxides To Sulfides With 1,3-Dithiane In The Presence Of Electrophilic Bromine As Catalyst. J Org Chem. 2002 May 3;67(9):2826-30.
合成参考文献
摘要:Molander, G. A.; Beaumard, F., Science of Synthesis Knowledge Updates, (2013) 3, 119. 摘要:Liu, Q., Science of Synthesis Knowledge Updates, (2014) 2, 277. 摘要:Ishii, A., Science of Synthesis Knowledge Updates, (2016) 2, 354. 摘要:Saikawa, Y.; Nakata, M., Science of Synthesis Knowledge Updates, (2018) 3, 381. 摘要:Saikawa, Y.; Nakata, M., Science of Synthesis Knowledge Updates, (2018) 3, 374.