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-5973161-A 优先权日:1996-03-18 标 题:Enantioselective synthesis of cyclopentenes 发明人:CRIMMINS MICHAEL T 权利人:UNIV NORTH CAROLINA 摘要:Methods of synthesizing compounds of the Formula V: ##STR1## wherein X c is a chiral auxiliary, m is from 1 to 4, and R 8 is hydrogen or --OH, are provided. n Additionally, methods of synthesizing compounds of the Formula XII: ##STR2## wherein m is from 1-4; B is hydrogen or a blocking group; and R 13 is a leaving group or a compound of formula R 14 --N--R 15 ; n wherein R 14 is hydrogen or branched or straight-chain C1-C6 alkyl; and R 15 is hydrogen, C3-C8 cycloalkyl, or branched or straight-chain alkyl; n are also provided. Novel compounds useful in the synthesis of cyclopentenes and carbocyclic nucleosides are further provided.
专利号:US-5446158-A 优先权日:1989-01-11 标题:Process for synthesis of FK-506 and tricarbonyl intermediates 发明人:JONES TODD K; MILLS SANDER G; ASKIN DAVID; REAMER ROBERT A; DESMOND RICHARD; TSCHAEN DAVID M; VOLANTE RALPH P; SHINKAI ICHIRO 权利人:MERCK & CO INC 摘要:A process is described for the total synthesis of the macrolide immunosuppressant, FK-506, and important tricarbonyl process intermediates thereof. The tricarbonyl intermediates can be produced by the mild oxidation of 2,3-dihydroxy carboxylate compounds containing olefin moieties.
专利号:US-7183059-B2 优先权日:1998-03-23 标 题 :Synthesis of compounds and libraries of compounds 发明人:VERDINE GREGORY L; CHYTIL MILAN; DIDIUK MARY T; MALINKY TIFFANY 权利人:HARVARD COLLEGE 摘要:A method of generating a compound having at least one biological activity of a peptide. The method includes identifying a biologically active peptide, providing a first monomer which contains terminal reactive moieties and at least one functionalizable group, providing a second monomer which contains terminal reactive moieties and at least one functionalizable group, and reacting first and second monomer under stereo-and/or regiochemically controlled conditions to yield a compound in which the monomers are attached by way of terminal reactive moieties.
专利号:US-5132457-A 优先权日:1991-08-26 标 题 :Stereospecific synthesis of 2(R)-2-methyl-3-dimethylamino-propiophenone (d-DAMP) 发明人:MATHEW JACOB 权利人:MALLINCKRODT SPEC CHEM 摘要:In a method for producing 2(R)-2-methyl-3-dimethylamino-propiophenone (d-DAMP), a chiral ester of the formula ##STR1## wherein R is an alkyl of from 1 to about 5 carbon atoms, is provided. The chiral easter of formula (I) is converted into a chiral amino-alcohol of the formula ##STR2## and the chiral amino-alcohol is oxidized so as to form d-DAMP.
专利号:US-11530204-B2 优先权日:2019-09-30 标 题 :Biocatalytic synthesis of cryptophycin anticancer agents 发明人:SHERMAN DAVID H; SCHMIDT JENNIFER J 权利人:UNIV MICHIGAN REGENTS 摘要:The disclosure provides cryptophycin intermediates, cryptophycin analogs, and cryptophycin chimeric molecules useful in treating cancer, as well as methods of producing these compounds and methods of treating cancer.
参考标题:Total Synthesis Of Rhizoxin D, A Potent Antimitotic Agent From The Fungus Rhizopus ChinensiS 作者:James D. White,Paul R. Blakemore,Neal J. Green,E. Bryan Hauser,Mark A. Holoboski,Linda E. Keown,Christine S. Nylund Kolz,Barton W. Phillips |发布日期:2002.11.1 摘要:Configuration At C5 Of 2 Through A Stereoselective Addition Of The Radical Derived From Dehalogenation Of 21 At The Beta Carbon Of The (Z)-Alpha,Beta-Unsaturated Ester. Aldehyde 29 Was Obtained From Phenylthioacetal 24 And Condensed With Phosphorane 30, Representing Subunit B, In A Wittig Reaction That Gave The (E,E)-Dienoate 31. This Ester Was Converted To Aldehyde 33 In Preparation For Coupling With
合成参考文献
摘要:Jie, X.; Su, W., Science of Synthesis, (2022) , 42. 摘要:Jie, X.; Su, W., Science of Synthesis, (2022) , 32.