专利号:US-7183417-B2 优先权日:2004-04-09 标题:Simple stereocontrolled synthesis of salinosporamide A 发明人:COREY ELIAS J 权利人:HARVARD COLLEGE 摘要:A simple and effective stereocontrolled synthesis of salinosporamide A(1) n nhas been developed which follows the pathway outlined in the FIGURE. The process, the first total synthesis of salinosporamide A, is capable of providing the compound in substantial quantities for further biological studies. In addition to the method of Scheme I, the present invention also includes several novel synthetic intermediate compounds, several intermediate steps of the preferred synthetic process; and the uses of these compounds in the preparation of synthetic derivatives of the compound Salinosporamide A. Salinosporamide A is of special interest as a synthetic target because of its protein in vitro cytotoxic activity against many tumor cell lines (IC 50 values of 10 nM or less).
专利号:US-2006287520-A1 优先权日:2005-05-16 标 题 :Synthesis of salinosporamide A and analogues thereof 发明人:DANISHEFSKY SAMUEL J; ENDO ATSUSHI 权利人:DANISHEFSKY SAMUEL J; ENDO ATSUSHI 摘要:A novel synthesis of salinosporamide A is provided. Salinospoamide A as well as structurally related natural products, omuralide and lactacystin, have been shown to be proteasome inhibitors. Therefore, these compounds as well as analogues of these natural products may be useful in the treatment of proliferative diseases such as cancer, autoimmune diseases, diabetic retinopathy, etc. The invention provides for the synthesis of salinosporamide A as well as analogs thereof using a convenient point for derivatization of the bicyclic core. Pharmaceutical compositions and method of using the inventive compounds are also provided.
专利号:US-4269772-A 优先权日:1980-01-14 标 题 :Synthesis of thienamycin via trans-3-carboxymethylene-4-carboxy-5-methyl-Δ2 -isoxazoline 发明人:MELILLO DAVID G; RYAN KENNETH M 权利人:MERCK & CO INC 摘要:Disclosed is a process for the stereocontrolled total synthesis of thienamycin, which synthesis proceeds via intermediate II: II wherein R5 and R6 are removable protecting groups.
专利号:US-6271379-B1 优先权日:2000-03-08 标题:Intermediates useful for the synthesis of huperzine A 发明人:TUECKMANTEL WERNER; KOZIKOWSKI ALAN P 权利人:UNIV GEORGETOWN 摘要:Intermediates useful for the synthesis of huperzine A represented by the structures below, n and methods for their synthesis, wherein: n R 1 is lower alkyl, benzyl, or substituted benzyl; n X is a suitable leaving group; n Y is an electron withdrawing group that can subsequently be converted into an amino group; n one broken line is present as a carbon—carbon bond and the other broken line is absent, where the broken line forms an unconjugated carbon—carbon double bond, which double bond may be endocyclic whereby n is 3 or the double bond may be exocyclic whereby n is 2.
专利号:US-7820838-B2 优先权日:2002-01-29 标 题:Method for total synthesis of ecteinascidins and intermediate compounds thereof 发明人:FUKUYAMA TOHRU; KAN TOSHIYUKI 权利人:JAPAN SCIENCE & TECH AGENCY 摘要:An intermediate compound for total synthesis of ecteinascidins comprising, a compound represented by general formula 2 having thioether group at C4 site, and the substituent R 2 of N 12 site is trichloroethoxycarbonyl (Troc) to which various substituents can be introduced by mild condition, further having 10 members ring structure which can be converted to a ring of other numbered members.
专利号:US-9346743-B2 优先权日:2012-10-15 标题 :Processes for the synthesis of 2-amino-4,6-dimethoxybenzamide and other benzamide compounds 发明人:THAKKAR AMIT; ZEILER ANDREW G; SKUFCA ANTHONY F; SPRINGER JAMES J; ASSINK BRYCE KELLY; LOZANOV MARIO E 权利人:ALBEMARLE CORP 摘要:This invention provides a method for the synthesis of a 2-amino-4,6-dimethoxybenzamide and other benzamides of Compound I: wherein R 1 , R 2 , R 3 , and R 4 each independently represent a hydrogen, a C 1 -C 6 alkyl, or a C 1 -C 6 alkoxy; and wherein R 6 and R 7 each independently represent a hydrogen, a C 1 -C 6 alkyl, a protecting group, or a directing group.
摘要:Sigma Aldrich; Product Search. Acetaldehyde oxime, mixture of syn and anti. Available from, as of May 20, 2013: 摘要:International Air Transport Association. Dangerous Goods Regulations. 47th Edition. Montreal, Quebec Canada. 2006., p. 131 摘要:49 CFR 171.2 (USDOT); U.S. National Archives and Records Administration's Electronic Code of Federal Regulations. Available from, as of August 12, 2013: 摘要:NIST; NIST Chemistry WebBook. Acetaldoxime (107-29-9). NIST Standard Reference Database No. 69, June 2005 Release. Washington, DC: US Sec Commerce. Available from, as of May 21, 2013: 摘要:U.S. Department of Transportation. 2012 Emergency Response Guidebook. Washington, D.C. 2012