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Author : Christina Goudreau Collison
Publisher :
ISBN 13 :
Total Pages : 358 pages
Book Rating : 4.:/5 (556 download)
Download or read book Studies Toward the Total Synthesis of ( - )-Apoptolidin written by Christina Goudreau Collison and published by . This book was released on 2004 with total page 358 pages. Available in PDF, EPUB and Kindle. Book excerpt:
Author : Bin Wu
Publisher :
ISBN 13 :
Total Pages : 550 pages
Book Rating : 4.:/5 (64 download)
Download or read book Studies Toward the Total Synthesis of Apoptolidin written by Bin Wu and published by . This book was released on 2004 with total page 550 pages. Available in PDF, EPUB and Kindle. Book excerpt:
Author : Gabriel N. Kapur
Publisher :
ISBN 13 : 9781109844450
Total Pages : 259 pages
Book Rating : 4.8/5 (444 download)
Download or read book Studies Directed Toward the Total Synthesis of (-)-apoptolidin written by Gabriel N. Kapur and published by . This book was released on 2006 with total page 259 pages. Available in PDF, EPUB and Kindle. Book excerpt: The northern hemisphere, which had been previously synthesized in our labs, was closely analyzed and synthesized again, with an improvement in the final three steps so that a more isomerically pure product resulted (15:1 now vs. 3:1 before). Finally, a crucial Suzuki coupling reaction of the northern and southern hemispheres was performed, which allowed the diol moiety at C19 and C20 to remain unprotected. This was followed by a saponification reaction to bring us to a very advanced carboxylic acid intermediate, one step from the closed 20-membered macrocycle.
Author : Venkatesan Srinivasan
Publisher :
ISBN 13 :
Total Pages : 872 pages
Book Rating : 4.:/5 (311 download)
Download or read book Studies Directed Toward the Total Synthesis of ( - )-apoptolidin A written by Venkatesan Srinivasan and published by . This book was released on 2008 with total page 872 pages. Available in PDF, EPUB and Kindle. Book excerpt:
Author : Douglas J. Tusch
Publisher :
ISBN 13 :
Total Pages : 240 pages
Book Rating : 4.:/5 (1 download)
Download or read book Part I. Studies Towards the Total Synthesis of (-)-Apoptolidin A ; Part II. Hydroxymethylation of Aldehydes and Its Application to (-)-Rasfonin written by Douglas J. Tusch and published by . This book was released on 2017 with total page 240 pages. Available in PDF, EPUB and Kindle. Book excerpt:
Author : Xiaorong Liu
Publisher :
ISBN 13 :
Total Pages : 524 pages
Book Rating : 4.:/5 (586 download)
Download or read book Studies on the Total Synthesis of ( - )-apoptolidin written by Xiaorong Liu and published by . This book was released on 2004 with total page 524 pages. Available in PDF, EPUB and Kindle. Book excerpt:
Author : Kyle William Rugg
Publisher :
ISBN 13 :
Total Pages : 307 pages
Book Rating : 4.:/5 (122 download)
Download or read book I. Second Generation Total Synthesis of (-)-Nakadomarin A written by Kyle William Rugg and published by . This book was released on 2018 with total page 307 pages. Available in PDF, EPUB and Kindle. Book excerpt: "Part I. The Second-Generation Total Synthesis of (-)-Nakadomarin A The second-generation total synthesis of (-)-nakadomarin A (1) has been described. A robust sequence toward the bicyclic lactam has been developed, allowing its production on > 5 g scale. This has been enabled by a number of significant improvements, including increased diastereoselectivity for the key SN2' cyclobutane formation, a scalable cyclobutanecarboximine formation/retro-aza-Claisen sequence, and the removal of a step from the longest-linear sequence by use of isocyanate addition to the bicyclic lactam in lieu of a two-step protocol. The Michael addition/spirocyclization's catalytic potential has been investigated, and a robust and scalable method for the synthesis of the spirocycle has been deployed. After pentacycle formation, macrocyclization, and reduction, (-)-nakadomarin A (1) is afforded with production of the target on over 0.5 g scale. This has resulted in a total synthesis of 1 in 16 steps (longest linear) and 6.5% overall yield. Part II. Studies Toward the Total Synthesis of (-)-Apoptolidin A A route toward the potent and selective apoptosis inducer (-)-apoptolidin A has been outlined. Production of the lactone comprising the southwestern quadrant of the natural product on scale by a previously described route has been investigated. Small-scale success in generating the lactone was ineffective on larger scales using the existing protocol due to the sensitive nature of an intermediate Diels-Alder adduct. Important advancement in material throughput was achieved by implementation of a robust two-step protocol for generating a critical intermediate alcohol on larger scales. Combined with the improvement of a deallylation protocol, a scalable route to the lactone of the southwestern quadrant of (-)-apoptolidin A has been established. With this, the completion of the southern hemisphere and aglycone of (-)-apoptolidin A will be accessible"--Pages x-xi.
Author : Bohan Jin
Publisher :
ISBN 13 :
Total Pages : 604 pages
Book Rating : 4.:/5 (519 download)
Download or read book Progress Towards the Total Synthesis of Apoptolidin written by Bohan Jin and published by . This book was released on 2002 with total page 604 pages. Available in PDF, EPUB and Kindle. Book excerpt:
Author : Lifeng Xiao
Publisher :
ISBN 13 :
Total Pages : 433 pages
Book Rating : 4.:/5 (111 download)
Download or read book I: Studies Toward the Total Synthesis of (-)-apoptolidin A written by Lifeng Xiao and published by . This book was released on 2017 with total page 433 pages. Available in PDF, EPUB and Kindle. Book excerpt: "Chapter 1: Studies toward the Total Synthesis of (-)-Apoptolidin A An approach to the total synthesis of the cell apoptosis inducer (-)-Apoptolidin A is described. Our synthetic strategy features the late installation of two sugar units on the core 20-membered macrocycle lactone which can be divided into two advanced subunits allowing for rapid convergence in the forward synthesis. Improvements to couple two subunits to afford the 20-membered macrocycle lactone, the synthesis of the third generation of the northern hemisphere vinyl bromide were developed. This approach involves a smooth transformation from crotyl alcohol to protected dialkyne in eight steps then finished the northern hemisphere through Suzuki coupling. Improvements to the synthesis of subunits vinyl iodide of the southern hemisphere through the synthesis of the bisalkyne subunit via bi-directional chain elongation of a C2 symmetric diepoxide as a key step were optimized. Chapter 2: Bone Targeted Bisphosphonate Conjugates with Releasable Payloads as Prodrugs for the Treatment of Bone Metabolic Diseases. Developments in studies of the invention of novel prodrugs for the treatment of bone metabolic diseases are described. Prodrugs are constituted with a bone selective bisphosphonate, variable linker moiety with bio-reversible carbamate linkage, and biological active parent drugs. These studies have been successful in developing: (1). Bisphosphonate-chloroquine conjugate for the treatment of osteoporosis and rheumatoid arthritis; (2). Bisphosphonate-bortezomib conjugate for the treatment of osteoporosis and multiple myeloma; (3). Bisphosphonate-GSI XII conjugate for the treatment of multiple myeloma; (4). Bisphosphonate-epigenetic inhibitor conjugates for the treatment of bone cancers; and (5). Bisphosphonate-fluorescent labeling conjugate for biologically mechanistic insight studies."--Pages xi-xii.
Author : Qingsong Liu
Publisher :
ISBN 13 :
Total Pages : pages
Book Rating : 4.:/5 (69 download)
Download or read book Large Scale Total Synthesis of Apoptolidinone and Progress Towards the Total Synthesis of Ammocidin written by Qingsong Liu and published by . This book was released on 2010 with total page pages. Available in PDF, EPUB and Kindle. Book excerpt: Apoptolidin 1.1 was isolated in 1997 by Hayakawa and co-workers from a soil bacterium Nocardiopsis sp. during screening for specific apoptosis inducers. The primary biological test revealed that this polyketide macrolide induced apoptosis in cells transformed with the adenovirus type E1A oncognene, but not normal cells. This dissertation describes the latest studies in understanding of apoptolidin's biological activity mechanism and previous contributions towards its total synthesis. Synthesizing apoptolidinone 1.26 by an intra-molecular Horner-Wadsworth-Emmons approach featuring a Suzuki coupling, cross metathesis and two diastereoselective aldol reactions is discussed. 15 mg apoptolidinone is prepared via our previously developed intramolecular Suzuking coupling approach. Ammocidin 3.1, which was found to induce apoptosis in Ba/F3-v12 cells in an IL- 3 free medium, is a specific apoptosis inducer discovered by Hayakawa and co-workers in 2001 from Saccharothrix sp. AJ9571. A strategy featuring Suzuki coupling, cross metathesis, Yamaguchi macrolactonization and three asymmetric aldol reactions was applied to the total synthesis of ammocidinone 3.6, the aglycone of ammocidin. The preparation of the key building blocks was discussed in the following chapter: aldehyde 3.8 (C14-C19) was synthesized via Sharpless asymmetric epoxidation; ethyl ketone 3.9' (C20-C28) was prepared via Kobayashi and Crimmins's asymmetric aldol methodologies; aldehyde 3.14 (C7-C13) was generated by Brown crotylation and cross metathesis.
Author : Karl A. Scheidt
Publisher :
ISBN 13 :
Total Pages : 652 pages
Book Rating : 4.3/5 ( download)
Download or read book I. Design and Synthesis of Cysteine Protease Inhibitors. II. Total Synthesis of (-)-bafilomycin A1 III. Studies Directed Towards the Total Synthesis of Apoptolidin written by Karl A. Scheidt and published by . This book was released on 1999 with total page 652 pages. Available in PDF, EPUB and Kindle. Book excerpt:
Author : Lars Volker Heumann
Publisher :
ISBN 13 :
Total Pages : 1920 pages
Book Rating : 4.:/5 (183 download)
Download or read book The Total Synthesis of Preswinholide and Studies Toward the Total Syntheses of Swinholide A and Acutiphycin written by Lars Volker Heumann and published by . This book was released on 2007 with total page 1920 pages. Available in PDF, EPUB and Kindle. Book excerpt:
Author : Yiwei Li
Publisher :
ISBN 13 :
Total Pages : pages
Book Rating : 4.:/5 (763 download)
Download or read book Total Synthesis of Apoptolidin and Synthesis of the Proposed Azaspiracid-1 Structure written by Yiwei Li and published by . This book was released on 2003 with total page pages. Available in PDF, EPUB and Kindle. Book excerpt: Discussed here in is the evolution of the strategies for the total synthesis of apoptolidin. Key features of this synthesis include the high levels of stereocontrol found in the crotyl- and allylborations, asymmetric dihydroxylation and aldol reaction to establish the required stereocenters. Stille and Suzuki coupling reactions, dithiane coupling reaction, Kahne's sulfoxide glycosidation and the highly efficient 1,2-thiophenyl migration/glycosidation were the keystones for the assembly of the building blocks. The synthetic efforts ultimately produced the first synthesis of this cytotoxic agent. Also described is the development of methodologies for the synthesis of the proposed azaspiracid-1 structure. The powerful synthetic technologies developed in this campaign, including the crucial two C-C bond-forming reactions, the novel dithiane coupling reaction and the sp2 - sp3 Stille coupling used to assemble the entire azaspiracid framework, stand out and will find applications in future synthetic efforts.
Author : William Vernier
Publisher :
ISBN 13 :
Total Pages : 202 pages
Book Rating : 4.:/5 (369 download)
Download or read book Studies Toward the Total Synthesis of Cylindrospermopsin written by William Vernier and published by . This book was released on 1997 with total page 202 pages. Available in PDF, EPUB and Kindle. Book excerpt:
Author : David Curtis Whritenour
Publisher :
ISBN 13 :
Total Pages : 608 pages
Book Rating : 4.:/5 (195 download)
Download or read book Studies Toward the Total Synthesis of Bryostatin 1 written by David Curtis Whritenour and published by . This book was released on 1988 with total page 608 pages. Available in PDF, EPUB and Kindle. Book excerpt:
Author : Sharlene Jolley
Publisher :
ISBN 13 :
Total Pages : 132 pages
Book Rating : 4.:/5 (4 download)
Download or read book Studies Toward the Total Synthesis of the Gonioheptolides written by Sharlene Jolley and published by . This book was released on 1998 with total page 132 pages. Available in PDF, EPUB and Kindle. Book excerpt:
Author : Jung-Nyoung Heo
Publisher :
ISBN 13 :
Total Pages : 458 pages
Book Rating : 4.:/5 (495 download)
Download or read book Synthetic Studies Toward the Total Synthesis of Ristocetin A written by Jung-Nyoung Heo and published by . This book was released on 2001 with total page 458 pages. Available in PDF, EPUB and Kindle. Book excerpt:
