专利号:US-11548898-B2 优先权日:2017-07-06 标题 :Synthesis of halichondrins 发明人:KISHI YOSHITO; AI YANRAN; YE NING; WANG QIAOYI; YAHATA KENZO; ISO Kentaro; NAINI SANTHOSH REDDY; YAMASHITA SHUJI; LEE JIHOON; OHASHI ISAO; FUKUYAMA TAKASHI 权利人:HARVARD COLLEGE; EISAI R&D MAN CO LTD 摘要:The present invention provides methods for the synthesis of ketones involving a Ni/Zr-mediated coupling reaction. The Ni/Zr-mediated ketolization reactions can be used in the synthesis of halichondrins (e.g., halichondrin A, B, C; homohalichondrin A, B, C; norhalichondrin A, B, C), and analogs thereof. Therefore, the present invention also provides synthetic methods useful for the synthesis of halichondrins, and analogs thereof. Also provided herein are compounds (i.e., intermediates) useful in the synthesis of halichondrins, and analogs thereof. In particular, the present invention provides methods and compounds useful in the synthesis of compound of Formula (H3-A).
专利号:US-6239313-B1 优先权日:2000-02-16 标 题 :Process for the solid state synthesis of enantiopure B-aminoalcohols from racemic epoxides 发明人:KAKULAPATI RAMA RAO; NANDURI BHANUMATHI; ELETI RAJENDER REDDY 权利人:COUNCIL SCIENT IND RES 摘要:The invention relates to a process for the solid state synthesis of enantiopure β-aminoalcohols by preparing inclusion complexes of aryloxyepoxide with cyclodextrin by adding an epoxide in equimolar ratio in an organic solvent to an aqueous solution of cyclodextrin, reacting the cyclodextrin complex of aryloxyepoxide with a nucleophile in solid state by intimately grinding the mixture using a mortar and pestle, continuing the mixing till the starting epoxide disappeared on tic, removing excess amines under vacuum, extracting the β-aminoalcohols produced with a solvent with yields of more than 50% and enantioselectivity of upto 100%.
专利号:US-5591852-A 优先权日:1990-08-10 标题 :Process for the preparation of nucleotides 发明人:VEMISHETTI PURUSHOTHAM; BRODFUEHRER PAUL R; HOWELL HENRY G; SAPINO JR CHESTER 权利人:ACAD OF SCIENCE CZECH REPUBLIC; REGA STICHTING 摘要:The present invention relates to a novel and economical process for the synthesis of HPMP-substituted nucleotide antiviral compounds. Also disclosed are novel intermediates produced in the process for the preparation of HPMPC.
专利号:US-2018111938-A1 优先权日:2015-05-05 标 题:Synthesis of Intermediates Used in the Manufacture of Anti-HIV Agents 发明人:PRADHAN BRAJA SUNDAR; AMARNATH KOMMIREDDY; VEMPALA NARESH; RAHMAN MD ATAUR 权利人:CBZ INVEST LTD 摘要:The present invention relates to a process of preparing intermediates of Formula (I). The process comprises of reacting compound of Formula (III) with compound of Formula (V) in the presence of a solvent selected from an alcohol, ether or water to form compound of Formula (I) wherein, R 1 is selected from —NH 2 , Cl, Br, NHCOR″, wherein R″ is alkyl, aryl, Schiff's base of formula Nâ• CHR′, wherein R′ is alkyl or aryl; R 2 is selected from H, alkyl; R 3 and R 4 , each independently is H; R 5 and R 6 , each independently is H, alkyl; R 7 is H, alkyl; and R 8 is H, alkyl.
专利号:RU-2185379-C2 优先权日:1996-01-25 标 题:Method of stereoselective synthesis of heterobicyclic alcohol enantiomer, intermediate compounds and methods of their synthesis
专利号:US-5935946-A 优先权日:1997-07-25 标 题 :Nucleotide analog composition and synthesis method 发明人:MUNGER JR JOHN D; ROHLOFF JOHN C; SCHULTZE LISA M 权利人:GILEAD SCIENCES INC 摘要:The invention provides a composition comprising bis(POC)PMPA and fumaric acid (1:1). The composition is useful as an intermediate for the preparation of antiviral compounds, or is useful for administration to patients for antiviral therapy or prophylaxis. The composition is particularly useful when administered orally. The invention also provides methods to make PMPA and intermediates in PMPA synthesis. Embodiments include lithium t-butoxide, 9-(2-hydroxypropyl) adenine and diethyl p-toluenesulfonylmethoxyphosphonate in an organic solvent such as DMF. The reaction results in diethyl PMPA preparations containing an improved by-product profile compared to diethyl PMPA made by prior methods.
[参考文献]: Troy D Haines, Et Al. Direct Determination Of Mcpd Fatty Acid Esters And Glycidyl Fatty Acid Esters In Vegetable Oils By Lc-Tofms. J Am Oil Chem Soc. 2011 Jan;88(1):1-14.
合成参考文献
摘要:Matsumoto, K.; Katsuki, T.; Arends, I. W. C. E., Science of Synthesis: Stereoselective Synthesis, (2011) 1, 70.