专利号:US-7423154-B2 优先权日:2001-03-07 标 题 :Asymmetric process for the preparation of diarylethylpiperazines derivatives and novel asymmetric diarylmethylamines as intermediates 发明人:BROWN WILLIAM; PLOBECK NIKLAS 权利人:ASTRAZENECA AB 摘要:An asymmetric synthesis of diarylmethylpiperazines is described. The synthetic route enables preparation of a variety of enatiomerically pure amines with different N-alkyl groups. The invention includes an asymmetric addition of organometallic compounds to chiral sulfinimine to give adducts in predominantly one diastereomer can subsequently be transferred into pure enantiomers of by cleavage of the chiral auxilliary which is followed by synthesis of the piperazine ring by alkylation procedures.
专利号:US-10759743-B2 优先权日:2016-10-24 标 题 :Pd-catalyzed γ-C(sp3)-H arylation / heteroarylation of free amines 发明人:YU JIN-QUAN 权利人:SCRIPPS RESEARCH INST 摘要:Pd(II)-catalyzed g-G(sp3)-H arylation or heteroarylation of primary amines is realized by using 2-hydroxynicotinaldehyde as a catalytic transient directing group. Importantly, the catalyst and the directing group loading can be lowered to 2% and 4% respectively, thus demonstrating high efficiency of this newly designed transient directing group. Heterocyclic aryl iodides are also compatible with this reaction. Furthermore, swift synthesis of 1,2,3,4-tetrahydronaphthyridine derivatives is accomplished using this reaction.
专利号:US-8299250-B2 优先权日:2007-10-18 标题:Chiral tridentate compounds, corresponding organometal complexes, method for preparing same and use of said compounds and complexes as ligands in asymmetrical catalysis 发明人:MAUDUIT MARC; RIX DIANE; CREVISY CHRISTOPHE; WENCEL JOANNA 权利人:MAUDUIT MARC; RIX DIANE; CREVISY CHRISTOPHE; WENCEL JOANNA; ECOLE NALE SUP ARTES METIERS; CENTRE NAT RECH SCIENT 摘要:The invention relates to a compound of the formula (I) or the formula (II) in which: W is an oxygen atom or a radical of the formula NH; X is hydrogen or an alkaline cation or a C1-C8 alkyl or a —(CH 2 ) n 3 —C(R 4 )(R 5 )(R 6 ) radical; X and R on the one hand and X and R 1 on the other hand may independently form an optionally substituted cycle with 5, 6 or 7 links. The invention also relates to complexes of said compounds with at least one metal selected from the group comprising copper, palladium, ruthenium, iridium and rhodium, and to a method for the synthesis of these compounds. These compounds and complexes can be used in various asymmetrical catalysis methods.
专利号:US-11117893-B2 优先权日:2018-09-24 标题 :Methods for preparation of substituted pyridines and related novel compounds 发明人:WATKINS EDMOND BLAKE; UREDI DILIPKUMAR; MOTATI DAMODER REDDY 权利人:WATKINS EDMOND BLAKE; UREDI DILIPKUMAR; MOTATI DAMODER REDDY; UNION UNIV 摘要:The present invention relates to novel methods of preparation of substituted pyridines and the compounds produced therefrom. In particular, the present invention provides efficient methods for the construction of diversely substituted pyridines, with varying substitution patterns under simple and metal-free conditions with high atom- and pot-economy and excellent functional group tolerance, and which are useful for the synthesis of natural products.
专利号:US-8378099-B2 优先权日:1994-10-28 标 题:Boronic ester and acid compounds, synthesis and uses 发明人:ADAMS JULIAN; MA YU-TING; STEIN ROSS L; BAEVSKY MATTHEW; GRENIER LOUIS; PLAMONDON LOUIS 权利人:MILLENNIUM PHARMACUETICALS INC; ADAMS JULIAN; STEIN ROSS L; BAEVSKY MATTHEW; GRENIER LOUIS; PLAMONDON LOUIS 摘要:Disclosed herein is a method for reducing the rate of degradation of proteins in an animal, comprising contacting cells of the animal with certain boronic ester and acid compounds. Also disclosed herein are novel boronic ester and acid compounds, their synthesis and uses.
专利号:CN-107417708-A 优先权日:2017-08-04 标 题 :A kind of water-soluble copper (II) complex and its synthesis method and application