专利号:US-9988349-B2 优先权日:2014-01-03 标 题:Direct stereospecific synthesis of unprotected aziridines from olefins 发明人:ESS DANIEL HALSELL; FALCK JOHN RUSSELL; JAT JAWAHAR LAL; KURTI LASZLO 权利人:ESS DANIEL HALSELL; FALCK JOHN RUSSELL; JAT JAWAHAR LAL; KURTI LASZLO 摘要:A method for the direct stereospecific conversion of structurally diverse mono-, di-, tri- and tetra-substituted olefins to N—H, N-alkyl, N-cycloalkyl, or N-aralkyl aziridines using a hydroxylamine amination agent with transition metal catalyst. The method is operationally simple (i.e., one-pot), scalable and fast at ambient temperature.
专利号:US-2006178357-A1 优先权日:2005-02-10 标题 :Chphalosporin-derived mercaptans as inhibitors of serine and metallo-beta-lactamases 发明人:BUYNAK JOHN D; CHEN HANSONG 权利人:BUYNAK JOHN D; CHEN HANSONG 摘要:Compounds of formula I: See Formula I in Figures Section n nwherein R 1 , R 2 , R 3 , R 4 and n have any of the values defined in the specification, and their pharmaceutically acceptable salts, are useful for inhibiting simultaneously serine and metallo-β-lactamase enzymes, for enhancing the activity of β-lactam antibiotics, and for treating β-lactam resistant bacterial infections in a mammal. The invention also provides pharmaceutical compositions, processes for preparing compounds of formula I, and novel intermediates useful for the synthesis of compounds of formula I.
专利号:US-7022691-B2 优先权日:2002-04-04 标题 :Inhibitors of serine and metallo-β-lactamases 发明人:BUYNAK JOHN D; CHEN HANSONG 权利人:BUYNAK JOHN D; CHEN HANSONG 摘要:Compounds of formula (I): n nwherein R 1 , R 2 , R 3 , R 4 and n have any of the values defined in the specification, and their pharmaceutically acceptable salts, are useful for inhibiting simultaneously serine and metallo-β-lactamase enzymes, for enhancing the activity of β-lactam antibiotics, and for treating β-lactam resistant bacterial infections in a mammal. The invention also provides pharmaceutical compositions, processes for preparing compounds of formula I, and novel intermediates useful for the synthesis of compounds of formula I.
专利号:US-7125986-B2 优先权日:1997-12-29 标题:Penicillanic acid derivative compounds and methods of making 发明人:BUYNAK JOHN D; RAO AKIREDDY SRINIVASA; DOPPALAPUDI VENKATA RAMANA 权利人:UNIV SOUTHERN METHODIST 摘要:Compounds of formula I: n nwherein R 1 , R 2 , R 3 , R 4 and n have any of the values defined in the specification, and their pharmaceutically acceptable salts, are useful for inhibiting β-lactamase enzymes, for enhancing the activity of β-lactam antibiotics, and for treating β-lactam resistant bacterial infections in a mammal. The invention also provides pharmaceutical compositions, processes for preparing compounds of formula I, and novel intermediates useful for the synthesis of compounds of formula I.
专利号:US-8207337-B2 优先权日:2007-01-29 标 题:Reagent for organic synthesis reaction containing organic triol borate salt 发明人:MIYAURA NORIO; YAMAMOTO YASUNORI 权利人:MIYAURA NORIO; YAMAMOTO YASUNORI; WAKO PURE CHEM IND LTD 摘要:[Problem] n To provide an organoboron compound-containing reagent for organic synthesis reactions which undergoes no trimerization with dehydration, does not necessitate activation with a base, and is stable and highly active. n [Means for Solving Problems] n The reagent for organic synthesis reactions contains an organic triol borate salt represented by any of the general formulae (I) to (III) and general formula (XVI): (wherein R 1 represents alkyl, alkenyl, etc.; R 2 represents optionally substituted alkyl, alkenyl, alkynyl, etc. or represents hydrogen; m + represents an alkaline metal ion, phosphonium ion, or given ammonium ion; M 2+ represents an alkaline earth metal; X represents halogen or alkoxide; Y represents an alkali metal ion, etc.; A represents optionally substituted methylene; and n represents an integer).
专利号:US-9493494-B2 优先权日:2014-05-30 标题:Phosphinine oxide derivative and preparation method thereof 发明人:LEE PHIL HO; PARK YOUNG CHUL; JEON IN CHEOL; SEO JUNG MIN; SEO BO RAM 权利人:KNU INDUSTRY COOPERATION FOUND 摘要:Provided are a novel phosphinine oxide derivative and a preparation method thereof, and more specifically, the phosphinine oxide derivative includes an oxaphosphinine oxide derivative and an azaphosphinine oxide derivative. n The phosphinine oxide derivative according to the present invention may have a pharmacological activity and a physiological activity, and may be used as a basic framework of a natural product and may be used for development of new drug and synthesis of various medical supplies. n In addition, according to the preparation method of the phosphinine oxide derivative according to the present invention, various phosphinine oxide derivatives with a high yield may be prepared by a simple synthesis process using an intramolecular annulation between a phosphinic derivative and an alkyne derivative in the presence of a rhodium (Rh) catalyst or a ruthenium (Ru) catalyst and an oxidant.