CAS: 104987-12-4; (3S,4R,5S,8R,9E,12S,14S,15R,16S,18R,19R,26As)-8-Ethyl-5,6,8,11,12,13,14,15,16,17,18,19,24,25,26,26A-Hexadecahydro-5,19-Dihydroxy-3-[(1E)-2-[(1R,3R,4R)-4-Hydroxy-3-Methoxycyclohexyl]-1-Methylethenyl]-14,16-Dimethoxy-4,10,12,18-Tetramethyl-15,19-Epoxy-3H-Py

上下游产品

24,33-bis-OTBDMS-ascomycin 11-epi-ascomycin 2(R),10(S),11(S)-cyclo-ascomycin 61H113NO12Si3C61H113NO12Si343H69NO12C43H69NO12 L 685818 33-(tert-butyldimethylsilyl)-24-deoxy-ascomycin 52H77NO14C52H77NO14

11-Epi-Ascomycin置于三乙胺体系中,用 乙腈 用作溶剂,化学反应生成长川霉素
参考文献:Selective Transformation Of Ascomycin Into 11-Epi-Ascomycin
标题:Selective Transformation Of Ascomycin Into 11-Epi-Ascomycin
摘要:Within The Binding Domain,Ascomycin Features The Unusual Pattern Of A Masked Tricarbonyl Moiety,Which Potentially Allows For High Structural Diversity Via Simple Isomerisation Events. A Cascade Of Diastereoselective Rearrangement Reactions At The Binding Domain,Allowing The Conversion Of Ascomycin Into 11-Epi-Ascomycin Is Herein Reported. (C) 2003 Elsevier Ltd. All Rights Reserved.
Doi:10.1016/j.Tetlet.2003.10.199

专利信息

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-9315483-B2
优先权日:2007-09-13
标题 :Synthesis of deuterated catechols and benzo[D][1,3]dioxoles and derivatives thereof
发明人：JONES ANDREW D; ZELLE ROBERT E; SILVERMAN I ROBERT
权利人:CONCERT PHARMACEUTICALS INC
摘要:The present invention provides a convenient and efficient process for the synthesis of d 2 -benzo[d][1,3]dioxoles.

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-8778636-B2
优先权日:2009-05-22
标题:Chemo-enzymatic approach to the synthesis of pimecrolimus
发明人：GRISENTI PARIDE; REZA ELAHI SHAHRZAD; VERZA ELISA
权利人:GRISENTI PARIDE; REZA ELAHI SHAHRZAD; VERZA ELISA; EUTICALS SPA
摘要:Processes for preparing pimecrolimus starting from ascomycin, exploiting the selectivity characteristics of the purified enzymatic systems particularly regarding the selective functionalization of the hydroxyl groups present in position 24 and 33 of ascomycin. Such method represents the first example of chemoenzymatic synthesis for preparing pimecrolimus.

专利号:US-6004787-A
优先权日:1991-01-17
标题:Method of directing biosynthesis of specific polyketides
发明人：KATZ LEONARD; DONADIO STEFANO; MCALPINE JAMES B
权利人:ABBOTT LAB
摘要:A method to produce novel polyketide structures by designing and introducing specified changes in the DNA governing the synthesis of the polyketide is disclosed. The biosynthesis of specific polyketide analogs is accomplished by genetic manipulation of a polyketide-producing microorganism by isolating a polyketide biosynthetic gene-containing DNA sequence, identifying enzymatic activities associated within the DNA sequence, introducing one or more specified changes into the DNA sequence which codes for one of the enzymatic activities which results in an altered DNA sequence, introducing the altered DNA sequence into the polyketide-producing microorganism to replace the original sequence, growing a culture of the altered microorganism under conditions suitable for the formation of the specific polyketide analog, and isolating the specific polyketide analog from the culture. The method is most useful when the segment of the chromosome modified is involved in an enzymatic activity associated with polyketide biosynthesis, particularly for manipulating polyketide synthase genes from Saccarharopolyspora or Streptomyces.

专利号:WO-9313663-A1
优先权日:1992-01-17
标 题:Method of directing biosynthesis of specific polyketides
发明人：KATZ LEONARD; DONADIO STEFANO; MCALPINE JAMES B
权利人:ABBOTT LAB
摘要:A method to produce novel polyketide structures by designing and introducing specified changes in the DNA governing the synthesis of the polyketide is disclosed. The biosynthesis of specific polyketide analogs is accomplished by genetic manipulation of a polyketide-producing microorganism by isolating a polyketide biosynthetic gene-containing DNA sequence, identifying enzymatic activities associated within the DNA sequence, introducing one or more specified changes into the DNA sequence which codes for one of the enzymatic activities which results in an altered DNA sequence, introducing the altered DNA sequence into the polyketide-producing microorganism to replace the original sequence, growing a culture of the altered microorganism under conditions suitable for the formation of the specific polyketide analog, and isolating the specific polyketide analog from the culture. The method is most useful when the segment of the chromosome modified is involved in an enzymatic activity associated with polyketide biosynthesis, particularly for manipulating polyketide synthase genes from Saccharapolyspora or Streptomyces.