专利号:US-9346853-B2 优先权日:2012-06-20 标 题 :Synthesis of telaprevir and boceprevir, or pharmaceutically acceptable salts or solvates as well as intermediate products thereof including β-amino acids prepared via Mukaiyama aldol addition 发明人:HOEFERL-PRANTZ KATHRIN; FELZMANN WOLFGANG; WILHELM THORSTEN; BENITO-GARAGORRI DAVID 权利人:SANDOZ AG 摘要:The invention relates to synthetic routes for preparing telaprevir and boceprevir, and its intermediates as well as peptides other than telaprevir. The synthetic routes are based on a Mukaiyama aldol addition reaction of a silyl enol ether or an enolate with an imine. The invention also refers to novel intermediates for preparing telaprevir/boceprevir or other peptides.
专利号:US-8008526-B2 优先权日:2005-03-17 标 题 :Synthesis reaction catalyst and method of synthesizing compound using the same 发明人:TANAKA HIROHISA; KANEKO KIMIYOSHI 权利人:DAIHATSU MOTOR CO LTD; HOKKO CHEM IND CO 摘要:To improve a catalytic activity of a composite oxide, to carry out a reaction in a high yield, and to provide a synthesis reaction catalyst having excellent handling properties and a method of a synthesizing a compound using the same, a synthesis reaction catalyst containing a palladium-containing perovskite-type composite oxide having a specific surface area of 0.5 to 9.5 m 2 /g is used in Suzuki Cross-Couplings given by the following general scheme (14).
专利号:WO-2006135646-A1 优先权日:2005-06-10 标题:Intermediates useful in the synthesis of alkylquinoline and alkylquinazoline kinase modulators and related methods of synthesis
专利号:EP-1891040-A1 优先权日:2005-06-10 标题 :Intermediates useful in the synthesis of alkylquinoline and alkylquinazoline kinase modulators and related methods of synthesis
专利号:US-7592473-B2 优先权日:2005-03-17 标题:Method of synthesizing compound 发明人:TANAKA HIROHISA; KANEKO KIMIYOSHI 权利人:DAIHATSU MOTOR CO LTD; HOKKO CHEM IND CO 摘要:In order to provide a method of synthesizing a compound in which activity of a catalyst is maintained even when the catalyst is recovered after the completion of the coupling reaction using a palladium-containing perovskite-type composite oxide as the catalyst and used repeatedly and the reaction can be carried out in a high yield, a palladium-containing perovskite-type composite oxide is used as a synthesis reaction catalyst and a reaction solvent containing an alkoxy alcohol is used as a reaction solvent in Suzuki Cross-Couplings given by the following general formula (15).
专利号:US-2015183824-A1 优先权日:2012-06-20 标 题 :SYNTHESIS OF TELAPREVIR AND BOCEPREVIR, OR PHARMACEUTICALLY ACCEPTABLE SALTS OR SOLVATES AS WELL AS INTERMEDIATE PRODUCTS THEREOF INCLUDING beta-AMINO ACIDS PREPARED VIA MUKAIYAMA ALDOL ADDITION
参考文献:10.1007/s00420-004-0523-4 摘要:Ben-Brik E, Jérôme L, Arnaud I, Yous S, Labat L, Haguenoer JM, Multigner L. Exposure to glycol ethers in a population of French men evaluated by measurement of urinary alkoxycarboxylic acids. International Archives of Occupational and Environmental Health. 2004 May 26;77(5):368–72. doi: 10.1007/s00420-004-0523-4. 参考文献:10.1539/joh.46.260 摘要:Choi HS, Park JH, Song JS, Cho YB. Determination of Urinary Metabolites of Alkyl Cellosolves by Solid Phase Extraction and GC/FID. Journal of Occupational Health. 2004 Jul;46(4):260–5. doi: 10.1539/joh.46.260.