共查询到20条相似文献,搜索用时 31 毫秒
1.
Paul S. Humphries Gayatri Balan Bruce M. Bechle Edward L. Conn Kenneth J. Dirico Yu Hui Robert M. Oliver James A. Southers Xiaojing Yang 《Tetrahedron letters》2009,50(18):2140-806
We have developed a number of efficient protocols for the facile synthesis of 1,2,3,4-tetrahydroisoquinolin-1-ones. This synthetic methodology allowed concise and efficient exploration of the SAR in all areas of the molecule. A number of these methods proved to be versatile, efficient and amenable to parallel synthesis. 相似文献
2.
Kong J Chen CY Balsells-Padros J Cao Y Dunn RF Dolman SJ Janey J Li H Zacuto MJ 《The Journal of organic chemistry》2012,77(8):3820-3828
A highly efficient synthesis of Vaniprevir (MK-7009) has been accomplished in nine linear steps and 55% overall yield. The key features of this synthesis include a cost-effective synthesis of the isoindoline subunit and efficient construction of the 20-membered macrocyclic core of Vaniprevir (MK-7009) utilizing ring-closing metathesis technology. A high-performing ring-closing metathesis protocol has been achieved by simultaneous slow addition of the ruthenium catalyst (0.2 mol %) and the diene substrate at a concentration of 0.13 M. 相似文献
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[reaction: see text] A concise and efficient synthesis of the permethyl derivative of the marine alkaloid ningalin C (2) has been accomplished. The key step involves the formation of a pyrrolinone from an aminoquinone in one pot. An efficient route for the synthesis of the key aminoquinone has also been developed. 相似文献
5.
A highly stereoselective and efficient asymmetric total synthesis of (+)-laurencin (1) has been accomplished from the known oxazolidinone 5 in 15 steps. The route features an efficient internal alkylation to form oxocene 3 from 4 and a novel use of acetonitrile anion as a two-carbon acetaldehyde equivalent for direct synthesis of ketone 2 from alpha-alkoxy amide 3. 相似文献
6.
Enantioselective Palladium‐Catalyzed Dearomative Cyclization for the Efficient Synthesis of Terpenes and Steroids
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Kang Du Pan Guo Yuan Chen Zhen Cao Dr. Zheng Wang Prof. Dr. Wenjun Tang 《Angewandte Chemie (International ed. in English)》2015,54(10):3033-3037
A novel enantioselective palladium‐catalyzed dearomative cyclization has been developed for the efficient construction of a series of chiral phenanthrenone derivatives bearing an all‐carbon quaternary center. The effectiveness of this method in the synthesis of terpenes and steroids was demonstrated by a highly efficient synthesis of a kaurene intermediate, the facile construction of the skeleton of the anabolic steroid boldenone, and the enantioselective total synthesis of the antimicrobial diterpene natural product (?)‐totaradiol. 相似文献
7.
An efficient approach to the total synthesis of the marine derived polypropionate cyercene A is described. A key feature of the synthesis is the development of methodology for the diastereoselective Wadsworth-Emmons type condensation of a functionalised γ-pyrone unit. 相似文献
8.
Apurba Bhattacharya Sankara Cherukuri Nitinchandra Patel John A. Grosso Venkatapuram A. Palaniswamy 《Tetrahedron letters》2006,47(31):5481-5484
A unique solvent effect encountered in the Barton-Zard pyrrole synthesis was exploited to develop an efficient synthesis of pyrrole-2-esters. The chemistry was extended to a one-pot synthesis of pyrrole-2,4-dicarboxylates. 相似文献
9.
《Angewandte Chemie (Weinheim an der Bergstrasse, Germany)》2017,129(26):7548-7551
A highly efficient synthesis of the enantioenriched tetrahydro‐β‐carbolines was developed by using a chiral phosphoric acid catalyzed Pictet–Spengler reaction of indolyl dihydropyridines. The reaction proceeds under mild reaction conditions to afford the desired chiral tetrahydro‐β‐carbolines in good to excellent yields (up to 96 %) and high enantioselectivities (up to 99 % ee ). With this method, a formal synthesis of tangutorine and a total synthesis of deplancheine were achieved in a highly efficient manner. 相似文献
10.
A short and efficient synthesis of enone 3, a key intermediate in the total synthesis of platencin (2), based on an intramolecular Diels-Alder reaction is described. 相似文献
11.
Reeves JT 《Organic letters》2007,9(10):1879-1881
A short and efficient total synthesis of the tripyrrole alkaloid butylcycloheptylprodigiosin is described. Key to the brevity of the approach is a two-step synthesis of macrocyclic formylpyrrole 4 from cyclononenone 6. 相似文献
12.
A practical and cost-effective synthesis of 3,3-difluoropyrrolidine is reported. The synthesis involves the isolation of two intermediates, which are prepared via two efficient through processes: (1) a Claisen rearrangement followed by a Ru(VIII)-catalyzed oxidation to prepare the 2,2-difluorosuccinic acid and (2) an efficient cyclization to form N-benzyl-3,3-difluoropyrrolidinone followed by BH(3).Me(2)S reduction. 相似文献
13.
[structure: see text]. An efficient, rapid synthesis of the A, B, C rings of terreulactone A is described. Key steps in the synthesis include a diastereoselective benzylic acid rearrangement to create the desired quaternary center at C2 and a mild bromolactonization to assemble the lactonic ring A. 相似文献
14.
A novel and efficient total synthesis of Englerin A is reported. The synthesis featured an intramolecular olefin metathesis ring closure reaction and a highly stereoselective oxygen bridge formation induced by an iodonium ion. This strategy can be used for the synthesis of natural products Englerin A and Englerin B and can provide flexibility in the preparation of various 9-substituted analogues of Englerin A for further structure–activity relationship studies. 相似文献
15.
G.B. Dharma RaoM.P. Kaushik 《Tetrahedron letters》2011,52(39):5104-5106
A simple and efficient trans-acetoacylation method for the synthesis of β-keto ester derivatives has been described using ytterbium(III) triflate as a new catalyst under solvent-free condition. This method was found to be efficient and convenient for the synthesis of a wide variety of β-keto ester derivatives. 相似文献
16.
[formula: see text] The first total synthesis of (+)-thiazinotrienomycin E (1), member of a novel class of cytotoxic ansamycin antibiotics, has been achieved. The synthesis features a highly efficient construction of the aromatic fragment 3 incorporating TBS protection of the aniline, a significantly improved synthesis of (-)-19, an intermediate employed in our trienomycins A and F total syntheses, application of the Kocienski modified Julia protocol to elaborate the E,E,E-triene subunit, an efficient union of 3 and (+)-4, and Mukaiyama macrolactamization to access the thiazinotrienomycin macrolide. 相似文献
17.
An efficient synthesis of the lactam core of pseurotin A has been accomplished. Key features of this synthesis include a tandem oxidation-cyclization to form the lactam from an acetylenic amide precursor. Although coupling of a lactam aldehyde with an appropriate side chain was not effective, it is anticipated that incorporating a partial side chain at an earlier stage should permit completion of the total synthesis of pseurotin A. 相似文献
18.
Janice CalzavaraJames McNulty 《Tetrahedron letters》2011,52(43):5672-5675
A short, convergent synthesis of the immunosuppressant FTY720 is described involving the use of 4-hydroxymethylbenzaldehyde as a pivotal intermediate. A double Wittig strategy was developed to connect this dual-functional aldehyde with an alkyl-tether and to a readily available TRIS-derivative leading to an efficient synthesis of the target molecule. 相似文献
19.
An efficient and concise approach to the synthesis of the macrolide core of the cryptophycins has been developed. A novel macrolactonization utilizing a reactive acyl-beta-lactam intermediate incorporates the beta-amino acid moiety within the 16-membered macrolide core. This modular approach, involving a cyanide-initiated acyl-beta-lactam ring opening followed by cyclization, was successfully applied to the total synthesis of cryptophycin-24. The strategy was also used in an efficient synthesis of the 6,6-dimethyl-substituted dechlorocryptophycin-52. In this case, the cyanide-initiated ring opening of the bis-substituted 2-azetidinone followed by macrolactonization was achieved through a catalytic process. 相似文献
20.
A new [2 + 2 + 2] approach to construct GPI molecules through the efficient synthesis of glucosamine-inositol and tetramannose intermediates led to a total synthesis of a GPI-anchor of Trypanosoma cruzi, and also afforded a key intermediate for the synthesis of valuable [4-deoxy-Man-III]-GPI analogues. 相似文献