专利号:US-2021107859-A1 优先权日:2018-04-06 标题 :A process for the synthesis of carbon labeled organic compounds 发明人:AUDISIO DAVIDE; CANTAT THIBAULT; DESTRO GIANLUCA 权利人:COMMISSARIAT ENERGIE ATOMIQUE 摘要:A process for the synthesis of a carbon labeled organic compound containing a carbon labeled carboxyl group is described. A method of using carbon labeled organic compounds containing a carbon labeled carboxyl group according to the present disclosure; a process for manufacturing labeled pharmaceuticals and agrochemicals comprising synthesis of carbon labeled organic compounds containing a carbon labeled carboxyl group according to the present disclosure; and a process for producing tracers comprising synthesis of carbon labeled organic compounds containing a carbon labeled carboxyl group according to the present disclosure are also described.
专利号:US-2004018598-A1 优先权日:2000-05-30 标题 :Bio-intermediates for use in the chemical synthesis of polyketides 发明人:SANTI DANIEL; ASHLEY GARY; MYLES DAVID C 摘要:The present invention relates to compounds made by a subset of modules from one or more polyketide synthase (“PKSâ€?) genes that are used as starting material in the chemical synthesis of novel molecules, particularly naturally occurring polyketides or derivatives thereof. The biologically derived intermediates (“bio-intermediatesâ€?) generally represent particularly difficult compounds to synthesize using traditional chemical approaches due to one or more stereocenters. In one aspect of the invention, an intermediate in the synthesis of epothilone is provided that feeds into the synthetic protocol of Danishefsky and co-workers. In another aspect of the invention, intermediates in the synthesis of discodermolide are provided that feed into the synthetic protocol of Smith and co-workers. By taking advantage of the inherent stereochemical specificity of biological processes, the syntheses of key intermediates and thus the overall syntheses of compounds like epothilone and discodermolide are greaty simplified.
专利号:US-6924385-B2 优先权日:2002-11-18 标 题:Method for synthesis of aliphatic isocyanates from aromatic isocyanates 发明人:LETTMANN CHRISTIAN; KOHLSTRUK STEPHAN; STOCHNIOL GUIDO; SPYROU EMMANOUIL 权利人:DEGUSSA 摘要:The invention relates to a method for synthesis of aliphatic isocyanates from aromatic isocyanates in substantially 3 stages. In particular, the invention relates to a method for synthesis of bis{4-isocyanatocyclohexyl}methane (H 12 MDI) from bis{4-isocyanatophenyl}methane (MDI). More especially, the invention relates to a method for synthesis of H 12 MDI with a trans-trans isomer content of <30%, preferably of <20%, particularly preferably of 5 to 15%.
专利号:US-2010143980-A1 优先权日:2007-02-22 标题:Synthesis of novel xylosides and potential uses thereof 发明人:BALAGURUNATHAN KUBERAN; MANIVANNAN ETHIRAJAN; XYLOPHONE V VICTOR; TRAN VY MY; NGUYEN KHIEM 权利人:BALAGURUNATHAN KUBERAN; MANIVANNAN ETHIRAJAN; XYLOPHONE V VICTOR; TRAN VY MY; NGUYEN KHIEM 摘要:The present invention includes a xyloside for use in inducing synthesis of a glycosaminoglycan in a cell, the xyloside having a chemical structure of one of Formula (1), Formula (2), Formula (3), Formula (4), Formula (5), Formula (6), Formula (7), Formula (8), Formula (9), or Formula (10) as shown herein. Also, the present invention includes a method of making a xyloside for use in inducing synthesis of a glycosaminoglycan in a cell, wherein the method is performed with “Clickâ€? chemistry. Additionally, the present invention includes a method of administering a xyloside so as to induce synthesis of a glycosaminoglycan in a cell.
专利号:US-2008086013-A1 优先权日:2006-06-15 标 题:Carbometallation of alkynes and improved synthesis of uniquinones 发明人:LIPSHUTZ BRUCE H 权利人:UNIV CALIFORNIA 摘要:Methods for the carbometallation of alkynes are presented. Those are useful for the synthesis of CoQ 10 and other ubiquinones as well as for the synthesis of ubiquinol analogs.
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.
[参考文献]: Alfonso Pérez-Garrido, Et Al. Convenient Qsar Model For Predicting The Complexation Of Structurally Diverse Compounds With Beta-Cyclodextrins. Bioorg Med Chem. 2009 Jan 15;17(2):896-904.
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