专利号:US-8410320-B2 优先权日:2010-12-07 标 题 :Method for synthesis of secondary alcohols 发明人:CHENG CHIEN-HONG; KARTHIKEYAN JAGANATHAN; HUANG PANG-CHI 权利人:CHENG CHIEN-HONG; KARTHIKEYAN JAGANATHAN; HUANG PANG-CHI; NAT UNIV TSING HUA 摘要:A method for synthesis of secondary alcohols is provided for pharmaceutical secondary alcohol by addition of organoboronic acids with aldehydes in presence of the cobalt ion and bidentate ligands as the catalyst. In addition, an enantioselective synthesis method for secondary alcohols is also herein provided in the present invention. The present invention has advantages in using less expensive cobalt ion and commercially available chiral ligands as the catalyst, wide scope of organoboronic acids and aldehydes compatible with this catalytic reaction and achieving excellent yields and/or enantiomeric excess.
专利号:US-2025188046-A1 优先权日:2023-12-08 标题:Ultrafast flow synthesis of functionalized sulfonyl fluorides and subsequent sufex connections via lithiated chemistry 发明人:KIM DONG-PYO; KANG JI-HO 权利人:POSTECH RES & BUSINESS DEV FOUND 摘要:Disclosed are ultrafast flow synthesis of functionalized sulfonyl fluorides and subsequent SuFEx connections via lithiated chemistry. In detail, a method of synthesizing an ortho-functionalized benzenesulfonyl fluoride derivative, the method comprises (a) reacting a benzenesulfonyl fluoride derivative represented by structural formula 1 with an organolithium represented by structural formula 2, thus synthesizing an intermediate represented by structural formula 3 in reaction scheme 1 and (b) reacting the intermediate with an electrophile, thus synthesizing a compound represented by structural formula 4 or a compound represented by structural formula 4′. The present disclosure enables the synthesis of several functionalized sulfonyl fluorides within a few seconds under mild temperature conditions in addition to the chemistry of Sulfonyl Fluoride Exchange (SuFEx), which is a next-generation click chemistry, so that sulfonyl fluoride, the main reactant of the SuFEx reaction, can be efficiently secured.
专利号:US-9242925-B2 优先权日:2011-08-29 标题:Versatile and stereospecific synthesis of γ,δ-unsaturated amino acids by Wittig reaction 发明人:JUGE SYLVAIN; BAYARDON JEROME; REMOND EMMANUELLE; ONDEL-EYMIN MARIE-JOELLE 权利人:JUGE SYLVAIN; BAYARDON JEROME; REMOND EMMANUELLE; ONDEL-EYMIN MARIE-JOELLE; CENTRE NAT RECH SCIENT; UNIV BOURGOGNE 摘要:The γ,δ-unsaturated α-amino acids of general formula (I). Also, a versatile process for the stereospecific synthesis of said compounds of formula (I), involving a Wittig reaction. Further, intermediate products of general formulae (II) and (III), as shown below, which are involved in the synthesis of compounds (I). n n n n n n n n n n n n Compounds of general formula (I) may be useful as therapeutic substances, or as reagents or intermediates for fine chemistry.
专利号:US-10266565-B2 优先权日:2011-04-12 标 题 :Peptide mimetic ligands of polo-like kinase 1 polo box domain and methods of use 发明人:BURKE JR TERRENCE R; LIU FA; LEE KYUNG S; PARK JUNG-EUN 权利人:BURKE JR TERRENCE R; LIU FA; LEE KYUNG S; PARK JUNG EUN; THE US SECRETARY DEPARTMENT OF HEALTH & HUMAN SERVICES 摘要:Novel compounds are provided that bind to polo-like kinases through the polo-box domain. In certain embodiments, the novel compounds are PEGylated peptides. The PEGylated peptides in accordance with the invention demonstrate high PBD-binding affinity. In certain embodiments, the PEGylated peptides have also achieved activities in whole cell systems. The invention also provides compounds that bind polo-like kinases through the polo-box domain and possess reduced anionic charge. Further provided are methods of design and/or synthesis of the PEGylated peptides and methods of use thereof. The invention provides methods of use of the compounds and methods of synthesis of the compounds.
专利号:US-8283502-B2 优先权日:2009-04-09 标题:Autocatalytic process for the synthesis of chiral propargylic alcohols 发明人:CHINKOV NICKA; WARM ALEKSANDER; CARREIRA ERICK 权利人:CHINKOV NICKA; WARM ALEKSANDER; CARREIRA ERICK; LONZA AG 摘要:An autocatalytic process for the synthesis of chiral propargylic alcohols.
专利号:WO-2014037963-A1 优先权日:2012-09-06 标 题 :A PROCESS FOR THE SYNTHESIS OF β, Æ´ UNSATURATED KETONES 发明人:MHASKE SANTOSH BABURAO; AHIRE MILIND MUKUND 权利人:COUNCIL SCIENT IND RES 摘要:The present invention disclose Pd/ N -Heterocyclic carbene catalyzed one step process for synthesis of β, Æ´-unsaturated ketones by direct acylation of allylic Carbons with aldehydes.