专利号:US-2025026768-A1 优先权日:2023-06-30 标题:Method for the synthesis of axially chiral organoboron compounds 发明人:PING YIFAN; CHE CHI-MING 权利人:LABORATORY FOR SYNTHETIC CHEMISTRY AND CHEMICAL BIOLOGY LTD 摘要:A highly efficient and atroposelective Rh-catalyzed [2+2+2] cycloaddition for the synthesis of axially chiral aryboron compounds is developed. The reactions of diynes and alkynylborons smoothly occur in an atom-economical manner, affording a variety of C—B atropisomers in excellent yields and enantioselectivities. The protocol features mild conditions, broad substrate scope, and good functional tolerance. The obtained C—B atropisomers show powerful synthetic applications in terms of producing novel chiral phosphine ligands.
专利号:US-12129222-B2 优先权日:2016-08-11 标题:Production of bitter principle derivatives 发明人:WYRWA RALF; RODE CLAUDIA; SEEMANN THOMAS; MEINEL LORENZ; RITZER JENNIFER; SCHNABELRAUCH MATTHIAS 权利人:UNIV WUERZBURG J MAXIMILIANS; JULIUS MAXIMILIANS UNIV 摘要:It is an object of the present invention to introduce carboxylic acid-functionalities suitable for coupling into the denatonium structure by means of simple synthesis, namely the synthesis of bitter principle derivatives based on the denatonium structure according to formula 1:For example, according to the invention, lidocaine derivatives may be reacted with carboxylated benzyl halogenides. The carboxylated denatonium derivatives of the present invention are especially applied in medicine, biology, medical engineering as well as cosmetics, the pharmaceutical, chemical, and foodstuff industry.
专利号:US-2024336559-A1 优先权日:2021-10-06 标 题 :Anti-fungals compounds targeting the synthesis of fungal sphingolipids 发明人:OJIMA IWAO; HARANAHALLI KRUPANANDAN; DEL POETA MAURIZIO; GARG ASHNA 权利人:UNIV NEW YORK STATE RES FOUND 摘要:The present invention provides a compound having the structure: n n n n n n n n n n n n wherein n R 3 , R 4 , R 5 , R 6 , and R 7 are each independently, H, halogen, CN, —CF 3 , —OCF 3 , —NO 2 , alkyl, alkenyl, alkynyl, aryl, heteroaryl, heterocycle, —OH, —OAc, —OR 13 , —COR 13 , —CH 2 OR 13 , —SH, —SR 13 , —SO 2 R 13 , —NH 2 , —NHR 13 , —NR 14 R 15 , —NHCOR 12 , or —CONR 14 R 15 ; n R 9 , R 10 , R 11 , and R 12 are each independently, H, CN, alkenyl, alkynyl, aryl, heteroaryl, cycloalkyl, heterocycloalkyl, —OAc, —COR 13 , —SH, —SR 13 , —SO 2 R 13 , —NH 2 , —NHR 13 , —NR 14 R 15 , —NHCOR 12 , or —CONR 14 R 15 ;n wherein each occurrence of R 13 is independently alkyl, alkenyl, alkynyl, aryl, or heteroaryl, wherein each occurrence of R 14 is independently —H, alkyl, alkenyl, alkynyl, aryl, or heteroaryl, wherein each occurrence of R 15 is independently —H, alkyl, alkenyl, alkynyl, aryl, or heteroaryl, n n wherein when R 14 is methyl, R 15 is not methyl; n wherein at least one of R 9 , R 10 , R 11 , and R 12 is not H; n wherein at least one of R 3 , R 4 , R 5 , R 6 , and R 7 is not H.
专利号:US-5932743-A 优先权日:1997-08-21 标 题:Methods for the solid phase synthesis of substituted indole compounds 发明人:COLLINI MICHAEL D; ELLINGBOE JOHN W 权利人:AMERICAN HOME PROD 摘要:The present invention relates to novel substituted indole compounds of formula (I) having pharmacological activity, to processes for their preparation, to solid phase methods for preparing libraries of the compounds, to utilizing libraries of the compounds for drug discovery, and to pharmaceutical compositions thereof.
专利号:US-8461298-B2 优先权日:2004-11-01 标 题:Compositions and methods for modification of biomolecules 发明人:BERTOZZI CAROLYN R; AGARD NICHOLAS J; PRESCHER JENNIFER A; BASKIN JEREMY MICHAEL 权利人:BERTOZZI CAROLYN R; AGARD NICHOLAS J; PRESCHER JENNIFER A; BASKIN JEREMY MICHAEL; UNIV CALIFORNIA 摘要:The present invention provides modified cycloalkyne compounds; and method of use of such compounds in modifying biomolecules. The present invention features a cycloaddition reaction that can be carried out under physiological conditions. In general, the invention involves reacting a modified cycloalkyne with an azide moiety on a target biomolecule, generating a covalently modified biomolecule. The selectivity of the reaction and its compatibility with aqueous environments provide for its application in vivo (e.g., on the cell surface or intracellularly) and in vitro (e.g., synthesis of peptides and other polymers, production of modified (e.g., labeled) amino acids).
专利号:WO-2021255429-A1 优先权日:2020-06-15 标题:Process for preparing n,n-dimethyl-4-((6-oxopyrimidin-1(6h)-yl)methyl)benzamide from 4-((6-oxopyrimidin-1(6h)-yl)methyl)benzoic acid, and crystalline forms of the benzamide 发明人:RAMSDEN NIGEL; FOX DAVID JOHN; TOMLINSON JAMES MICHAEL 权利人:Z FACTOR LTD 摘要:The invention includes a process for the synthesis of N,N-dimethyl-4-((6-oxopyrimidin-1(6H)- yl)methyl)benzamide and 4-((6-oxopyrimidin-1(6H)-yl)methyl)benzoic acid, a process for 5 synthesising crystalline forms of N,N-dimethyl-4-((6-oxopyrimidin-1(6H)- yl)methyl)benzamide, and crystalline forms of N,N-dimethyl-4-((6-oxopyrimidin-1(6H)- yl)methyl)benzamide.
[参考文献]: Jin-Xiang Chen, Et Al. Synthesis, Characterization And Potent Dna-Cleaving Activity Of Copper(Ii)-Complexed Berberine Carboxylate. Bioorg Med Chem Lett. 2012 Dec 1;22(23):7056-9.
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