专利号:US-7368568-B2 优先权日:2001-08-03 标 题 :Protected 3,5-dihydroxy-2,2-dimethyl-valeroamides for the synthesis of epothilones and derivatives and process for production and the use 发明人:WESTERMANN JURGEN; PLATZEK JOHANNES; PETROV ORLIN 权利人:BAYER SCHERING PHARMA AG 摘要:The invention relates to new protected 3,5-dihydroxy-2,2-dimethyl-valeroarnides for the synthesis of edothilones and derivatives and process for the production and the use of the new compounds for the production of epothilones or epothilone derivatives.
专利号:US-6933385-B2 优先权日:2001-08-03 标题 :Protected 3,5-dihydroxy-2,2-dimethyl-valeroamides for the synthesis of epothilones and derivatives and process for the production and the use 发明人:WESTERMANN JURGEN; PLATZEK JOHANNES; PETROV ORLIN 权利人:SCHERING AG 摘要:The invention relates to new protected 3,5-dihydroxy-2,2-dimethyl-valeroamides for the synthesis of epothilones and derivatives and process for the production and the use of the new compounds for the production of epothilones or epothilone derivatives.
专利号:US-4412958-A 优先权日:1981-10-16 标 题:Stereospecific synthesis of 5-phenyl-2S-pentanol 发明人:CUE JR BERKELEY W; MOORE BERNARD S 权利人:PFIZER 摘要:5-Phenyl-2S-pentanol is synthesized stereospecifically from S ethyl lactate. The method provides easily purified 5-phenyl-2S-pentanol useful in the synthesis of central nervous system active (CNS) agents such as levonantradol.
专利号:US-7442802-B2 优先权日:2002-06-27 标 题:Cyclooxygenase-2 selective inhibitors, compositions and methods of use 发明人:BANDARAGE UPUL K; EARL RICHARD A; EZAWA MAIKO; FANG XINQIN; GARVEY DAVID S; KHANAPURE SUBHASH P; RANATUNGE RAMANI R; RICHARDSON STEWART K; SCHROEDER JOSEPH D; STEVENSON CHERI A; WEY SHIOW-JYI 权利人:NITROMED INC 摘要:The invention describes novel cyclooxygenase 2 (COX-2) selective inhibitors and novel compositions comprising at least one cyclooxygenase 2 (COX-2) selective inhibitor, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase, and/or at least one therapeutic agent. The invention also provides novel kits comprising at least one COX-2 selective inhibitor, optionally nitrosated and/or nitrosylated, and, optionally, at least one nitric oxide donor, and/or, optionally, at least one therapeutic agent. The novel cyclooxygenase 2 selective inhibitors of the invention can be optionally nitrosated and/or nitrosylated. The invention also provides methods for treating inflammation, pain and fever; for treating and/or improving the gastrointestinal properties of COX-2 selective inhibitors; for facilitating wound healing; for treating and/or preventing renal and/or respiratory toxicity; for treating and/or preventing other disorders resulting from elevated levels of cyclooxygenase-2; and for improving the cardiovascular profile of COX-2 selective inhibitors.
专利号:US-6335458-B1 优先权日:1998-02-27 标题:Intermediate compounds in the synthesis of the A ring moiety of 2-substituted vitamin D derivatives 发明人:OGASAWARA KUNIO; TAKAHASHI MICHIYASU 权利人:CHUGAI PHARMACEUTICAL CO LTD 摘要:The object of the present invention is to provide novel compounds corresponding to the A ring part of vitamin D derivatives having a substituent at the 2-position. According to the present invention, there are provided compounds of the general formula (1):(wherein R1, R2 and R3, which may be the same or different, represent a hydrogen atom or a protecting group and R4 represents a lower alkyl group), intermediates for synthesizing them and a process for preparing them.
专利号:US-6989401-B2 优先权日:2000-07-19 标题:Sulfonic acid derivatives of hydroxamic acids and their use as medicinal products 发明人:MAEDA KAZUHIRO; SONDA SHUJI; TAKEMOTO TADAHIRO; GOTO TOMOKAZU; KOBAYASHI FUJIO; KAJII MASAHIKO; KOMORITA NARUYASU; HIRAYAMA FUMIHIRO 权利人:MITSUBISHI PHARMA CORP 摘要:The present invention relates to a novel sulfonic acid derivative of hydroxamic acid or a pharmacologically acceptable salt thereof. More particularly, the present invention relates to a sulfonic acid derivative of hydroxamic acid or a pharmacologically acceptable salt thereof, which is useful as an inhibitor of lipopolysaccharides (LPS). In addition, the present invention relates to a novel intermediate compound useful for the synthesis of this sulfonic acid derivative of hydroxamic acid.
[参考文献]: Cheng Chen, Et Al. Selective Catalytic Sp3 C-O Bond Cleavage With C-N Bond Formation In 3-Alkoxy-1-Propanols. Org Lett. 2012 Jun 15;14(12):2992-5. [参考文献]: Douglas M Mans, Et Al. Total Synthesis Of (+)-Cocaine Via Desymmetrization Of A Meso-Dialdehyde. Org Lett. 2004 Sep 16;6(19):3305-8.
合成参考文献
摘要:Podlech, J., Science of Synthesis Knowledge Updates, (2018) 4, 137. 摘要:Margaretha, P., Science of Synthesis Knowledge Updates, (2014) 2, 437. 摘要:Arndtsen, B. A.; Tjutrins, J., Science of Synthesis: Multicomponent Reactions, (2013) 2, 517. 摘要:Sasano, Y.; Iwabuchi, Y., Science of Synthesis: Special Topics, (2022) 1, 329.