专利号:US-10053406-B2 优先权日:2015-10-23 标题 :Synthesis of honokiol 发明人:JARACZ STANISLAV; KOZLOWSKI MARISA; EUN LEE YOUNG; KIM SUN MIN 权利人:COLGATE PALMOLIVE CO; UNIV PENNSYLVANIA 摘要:Disclosed herein are improved methods for the synthesis of honokiol, as well as methods for the synthesis of 3,3′-di-tert-butyl-5,5′-dimethyl-[1,1′-biphenyl]-2,4′-diol, 3′,5-dimethyl-[1,1′-biphenyl]-2,4′-diol, and 2,4′-dimethoxy-3′,5-dimethyl-1,1′-biphenyl, 3,3′,5,5′-tetra-tert-butyl-[1,1′-biphenyl]-2,4′-diol, and certain tetrasubstituted bisphenols, and uses therefor.
专利号:US-9783549-B2 优先权日:2013-11-04 标题:Macrocyclization reactions and intermediates useful in the synthesis of analogs of halichondrin B 发明人:FANG FRANCIS G; KIM DAE-SHIK; CHOI HYEONG-WOOK; CHASE CHARLES E; LEE JAEMOON 权利人:EISAI R&D MAN CO LTD 摘要:The invention provides methods for the synthesis of eribulin or a pharmaceutically acceptable salt thereof (e.g., eribulin mesylate) through a macrocyclization strategy. The macrocyclization strategy of the present invention involves subjecting a non-macrocyclic intermediate to a carbon-carbon bond-forming reaction (e.g., an olefination reaction (e.g., Homer-Wadsworth-Emmons olefination), Dieckmann reaction, catalytic Ring-Closing Olefin Metathesis, or Nozaki-Hiyama-Kishi reaction) to afford a macrocyclic intermediate. The invention also provides compounds useful as intermediates in the synthesis of eribulin or a pharmaceutically acceptable salt thereof and methods for preparing the same.
专利号:US-2010312013-A1 优先权日:2009-06-03 标 题:Steroselective synthesis of certain trifluoromethyl-substituted alcohols 发明人:FANDRICK DANIEL R; YEE NATHAN K; SONG JINHUA J; REEVES JONATHAN T 权利人:BOEHRINGER INGELHEIM INT 摘要:A process for synthesis of a compound of Formula (X) n n n n n n n n n n wherein:n R 1 is an aryl group substituted with one to three substituent groups,n wherein each substituent group of R 1 is independently C 1 -C 5 alkyl, aminocarbonyl, alkylaminocarbonyl, dialkylaminocarbonyl, halogen, carboxy, cyano, or trifluoromethyl,n wherein each substituent group of R 1 is optionally independently substituted with one to three substituents selected from C 1 -C 3 alkyl, C 1 -C 3 alkoxy, phenyl, and alkoxyphenyl; and n n R 2 and R 3 are each independently C 1 -C 5 alkyl.
专利号:US-4922049-A 优先权日:1989-01-13 标 题:Synthesis of cis-olefins 发明人:BYERS JIM D 权利人:PHILLIPS PETROLEUM CO 摘要:A process for the synthesis of cis-olefins from cis-olefinic alcohols consisting essentially of the following steps: n (a) reacting a cis-olefinic alcohol with a source of an alkali metal ion selected from the group consisting of lithium and sodium ions to form a first reaction product, n (b) then contacting said thus formed first reaction product with a sulfonyl halide compound to form a second reaction product, n (c) then containing said thus formed second reaction product with an alkyl magnesium compound and a cuprous salt to form a third reaction product comprising a cis-olefin wherein said steps are carried out in a suitable organic solvent.
专利号:US-4365094-A 优先权日:1979-12-28 标 题 :Process for the synthesis of tertiary phosphine oxides, and new tertiary phosphine oxides 发明人:BOILEAU SYLVIE L; N GUYEN THANH-DUNG; GAUTIER JEAN-CLAUDE C 权利人:POUDRES & EXPLOSIFS STE NALE 摘要:The invention relates to the synthesis of tertiary phosphine oxides and also to certain tertiary phosphine oxides. According to the invention, an organic phase containing a halogenomethyl derivative, a secondary phosphine oxide and a phase transfer catalyst in an organic medium is reacted with an aqueous phase containing an inorganic base. The halogenomethyl derivative can be a micromolecule or a macromolecule. The tertiary phosphine oxides are substances which are useful, in particular, in fireproofing, in hydrometallurgy and in the field of plant health.
专利号:US-5789576-A 优先权日:1994-12-09 标题 :Methylphosphonate dimer synthesis 发明人:DAILY WILLIAM J; SCHWARTZ DAVID AARON 权利人:GENTA INC 摘要:Processes for the stereospecific synthesis of 2',2''-bis(deoxy)di-nucleosides and for the stereoselective synthesis of 2',2''-bis(substituted) dinucleosides are provided. Also provided are activated 2'-substituted-nucleoside alkylphosphonate active esters useful in the synthesis of these dinucleosides.