专利号:WO-2017080770-A1 优先权日:2015-11-10 标题 :Synthesis of (z)-endoxifen hydrochloride 发明人:HEINKELE GEORG; MUERDTER THOMAS; SCHWAB MATTHIAS 权利人:ROBERT BOSCH GES FÜR MEDIZINISCHE FORSCHUNG MBH 摘要:The invention relates to the synthesis of tamoxifen, endoxifen and derivatives thereof. Starting from a substituted benzoic acid derivative and 2-phenoxyethyl halide, the intermediate product of general formula (I) is obtained. The compound of general formula (VI) or a salt thereof is obtained from the compound of general formula (I), via isomer purification of the compound of general formula (I) by obtaining the (Z)-isomers and reacting the (Z)-isomers with an amine of formula HNR 6 R 7 . Alternatively, the compound of general formula (I) is reacted with a compound of formula HNR 6 R 7 , and the amine thus obtained is then subjected to isomer purification, wherein the compound of general formula (VI) or a salt thereof is obtained.
专利号:US-8912150-B2 优先权日:2001-08-03 标题:Ribosome structure and protein synthesis inhibitors 发明人:STEITZ THOMAS A; MOORE PETER B; SUTCLIFFE JOYCE A; OYELERE ADEGBOYEGA K; IPPOLITO JOSEPH A 权利人:RIB X PHARMACEUTICALS INC; UNIV YALE; MELINTA THERAPEUTICS INC 摘要:The invention provides methods for producing high resolution crystals of ribosomes and ribosomal subunits as well as crystals produced by such methods. The invention also provides high resolution structures of ribosomal subunits either alone or in combination with protein synthesis inhibitors. The invention provides methods for identifying ribosome-related ligands and methods for designing ligands with specific ribosome-binding properties as well as ligands that may act as protein synthesis inhibitors. Thus, the methods and compositions of the invention may be used to produce ligands that are designed to specifically kill or inhibit the growth of any target organism.
专利号:US-7385064-B1 优先权日:2005-11-30 标题 :Catalysts for use in enantioselective synthesis 发明人:DAVIES HUW M L; REDDY RAVISEKHARA P 权利人:UNIV NEW YORK STATE RES FOUND 摘要:Disclosed are compounds having the following formula: n nin which Z 11 is selected from a substituted or unsubstituted saturated adamantyl or other polycyclic group and a substituted or unsubstituted branched acyclic group containing at least 5 carbon atoms at least one of which is a tertiary carbon; and in which Z 12 is a cyclic imide. Methods of using these compounds as chiral catalysts for carbenoid reactions and for enantioselective C—H aminations are also described.
专利号:US-5202444-A 优先权日:1990-11-27 标题:Optically isomeric inositol and process for making optically active compound 发明人:OZAKI SHOICHIRO; AKIYAMA TAKAHIKO; KAGEYAMA KUNIO; MACHIDA MORIHISA 权利人:YOKOHAMA RUBBER CO LTD 摘要:Optically active diols and hydroxycarboxylic acids and their esters are produced by deriving 1L-1,2:5,6-di-O-cyclohexylidene-chiro-inositol from 1L-chiro-inositol as an asymmetric source, followed by introduction of a selected class of sterically hindering and asymmetrically reactive groups into the first-mentioned compound and by subsequent reduction of the resulting compound. Seven specific inositols are also derivable from synthesis of those ultimate compounds.
专利号:US-4269773-A 优先权日:1976-04-27 标 题:Fused oxazolidine compounds 发明人:MITSURU YOSHIOKA; TERUJI TSUJI; YASUHIRO NISHITANI; WATARU NAGATA 权利人:SHIONOGI & CO 摘要:Compounds represented by the following formula prepared from 6-aminopenicillanic acid are key intermediates in a stereo-specific synthesis of 1-oxadethiacephalosporins, highly active antibiotics: +TR [wherein COA and COB each is carboxy or protected carboxy; COX is carboxy, protected carboxy, or a group of the formula -COCQ=N2 or -COCHQ-Z (in which Q is hydrogen, lower alkyl or aryl; and Z is hydrogen or a nucleophilic group); Hal is halogen; R is lower alkyl or aralkyl; and Y is hydrogen or acyl].
专利号:DE-102015222031-A1 优先权日:2015-11-10 标题 :Synthesis of (Z) -endoxifene hydrochloride
参考标题:Synthesis Of Pyrido[2,3‐ B ]Indole Derivatives Via Rhodium‐catalyzed Cyclization Of Indoles And 1‐sulfonyl‐1,2,3‐triazoles 作者:Shengguo Duan,Yuehui An,Bing Xue,Yidian Chen,Wan Zhang,Ze‐feng Xu,Chuan‐ying Li |发布日期:2020.4.27 摘要:Acyloxy‐substituted α,β‐unsaturated Imines Generated In Situ From Triazoles Can Act As Aza‐[4 C] Synthons And Be Trapped By Indoles In A Stepwise [4 + 2] Cycloaddition Reaction, Thus Providing Rapid Access To Valuable Pyrido[2,3‐b]Indoles In High Yields. Attractive Features Of This Reaction System Include Operational Simplicity, Readily Available Substrates, Construction Of Sterically Demanding Quaternary
合成参考文献
摘要:Schafer, E. W., Jr., and W. A. Bowles Jr. 1985. Acute oral toxicity and repellency of 933 chemicals to house and deer mice. Archives of Environmental Contamination and Toxicology 14:111-129. https://www.aphis.usda.gov/ws/nwrc/chem-effects-db/S_schafer851.pdf