专利号:US-7173059-B2 优先权日:2003-05-08 标题:Intermediates useful in the synthesis of HIV-protease inhibitors and methods for preparing the same 发明人:ALBIZATI KIM FRANCIS; BABU SRINIVASAN 权利人:AGOURON PHARMA 摘要:Optically active 3-amino-butene and 1,2-dihydroxy-3-amino-butane intermediate compounds, useful in the synthesis of HIV-protease inhibitors and methods of preparing these intermediate compounds are disclosed.
专利号:WO-9516049-A1 优先权日:1993-12-08 标题 :Catalytic chemo-enzymatic asymmetric synthesis of carbohydrates 发明人:WONG CHI-HUEY; SHARPLESS BARRY K 权利人:SCRIPPS RESEARCH INST; WONG CHI HUEY; SHARPLESS BARRY K 摘要:A stereoselective synthesis of carbohydrates employs two key stereoselective steps, viz. an osmium-catalyzed asymmetric dihydroxylation (AD) of an alkene to form an aldol intermediate and an aldolase-catalyzed aldol addition reaction wherein the aldol intermediate is elongated by the addition of a ketone. Moreover, ketoses having four new stereocenters can be synthesized without the use of chiral starting materials. The stereoselectivity of the asymmetric dihydroxylation (AD) reaction is determined by the cis or trans (Z or E) stereoisomeric configuration of the alkene and by the choice of AD-mix, i.e., an AD-mix-α or AD-mix-β. The stereoselectivity of the aldolase-catalyzed addition reaction is determined by the choice of aldolase and by the stereochemistry of the aldol intermediate. Four aldolases with broad substrate specificity are sufficient to produce all possible enantiomeric combinations of the two hydroxymethylene stereocenters formed during the aldol addition reaction. Accordingly, a synthetic scheme combining an osmium-catalyzed asymmetric dihydroxylation (AD) reaction and an aldolase-catalyzed aldol addition reaction enables direct access to a wide range of carbohydrate derivatives containing up to four new hydroxymethylene stereocenters.
专利号:US-9902699-B2 优先权日:2012-10-24 标题 :Synthesis of tetrahydroisoquinolines from 2-methyl-1-phenyl substituted indenes 发明人:ROSOCHA GREGORY; BATEY ROBERT 权利人:ROSOCHA GREGORY; Gregory Rosocha 摘要:A procedure for the synthesis of tetrahydroisoquinolines from 2-methyl-1-phenyl substituted indene is described. The process involves the use of osmium tetroxide to cleave the indene double bond forming the keto aldehyde product, which is then combined with a substituted amine forming the substituted isoquinoline. Isoquinolines can be useful as industrial products in the chemical, agrochemical, oil and gas industry, as well as useful as medicaments in the pharmaceutical industry.
专利号:US-9505733-B2 优先权日:2011-11-18 标题:Single step enantioselective process for the preparation of 3-substituted chiral phthalides 发明人:REDDY REKULA SANTOSH; NAGA CHITHANYA KIRAN INDUKURU; ARUMUGAM SUDALAI 权利人:COUNCIL SCIENT IND RES 摘要:The present invention discloses single step, highly enantioselective catalytic oxidative cyclization process for the synthesis of 3-substituted chiral phthalides. In particular, the invention discloses asymmetric synthesis of chiral phthalides via synergetic nitrile accelerated oxidative cyclization of o-cyano substituted aryl alkenes in high yield and enantiomeric excess (ee) in short reaction time. Also, disclosed herein is “one-pot†asymmetric synthesis of biologically important natural compounds having 3-substituted chiral phthalide structural framework in the molecule.
专利号:US-11976081-B2 优先权日:2019-04-26 标题 :Intermediate of eribulin and synthesis method and use thereof 发明人:XU WEIPING 权利人:BEIJING TIENYI LUFU PHARMATECH CO LTD 摘要:An intermediate compound is prepared and used for the synthesis of halichondrin B, eribulin or an analog thereof, particularly a structural fragment C27-C35 thereof. The starting materials of the synthetic route are readily available, and the optical purity of the starting materials can be ensured, so that the optical purity of the structural fragment C27-C35 in halichondrin B, eribulin or the analog thereof is ensured. Steps for constructing a chiral center of the structural fragment C27-C35 feature higher diastereoselectivity and yield, in particular preparation methods of compounds of formulae (X), (XI), (XVI) and (XV). By-products of partial reactions can be removed only by recrystallization, which results in easy purification and significant reduce in cost.
专利号:US-11466046-B2 优先权日:2014-10-08 标题 :14-membered ketolides and methods of their preparation and use 发明人:MYERS ANDREW G; SEIPLE IAN BASS; ZHANG ZIYANG 权利人:HARVARD COLLEGE 摘要:Provided herein are methods of preparing new 14-membered ketolides via coupling of an eastern and western half moiety, followed by macrocyclization, and optional functionalization. Intermediates in the synthesis of these ketolides including the eastern and western halves are also provided. Pharmaceutical compositions and methods of treating infectious diseases and inflammatory conditions using these ketolides are also provided.
摘要:Wong, Y.-S., Science of Synthesis, (2009) 46, 630. 摘要:Camp, J. E., Science of Synthesis Knowledge Updates, (2012) 1, 347. 摘要:Poechlauer, P.; Zimmermann, A., Science of Synthesis: Catalytic Reduction in Organic Synthesis, (2017) 1, 327.