STILLE CROSS-COUPLING REACTIONS OF ARYL MESYLATES AND TOSYLATES USING A BIARYLPHOSPHINE BASED CATALYST SYSTEM [0.03%]
一类新型双芳基膦配体催化的芳基甲磺酸酯和对甲苯磺酸酯的交叉偶联反应
John R Naber,Brett P Fors,Xiaoxing Wu et al.
John R Naber et al.
A catalyst system for the Stille cross-coupling reactions of aryl mesylates and tosylates is reported. Using the combination of Pd(OAc)2, XPhos, and CsF in t-BuOH an array of aryl and heteroaryl sulfonates were successfully employed in thes...
MILD AND SELECTIVE O-GLYCOSYLATIONS OF PRIMARY ALCOHOLS WITH THE THIOGLUCOSAMINIDE DERIVATIVE PROMOTED BY N-IODOSUCCINIMIDE AND HBF(4)-ADOSROBED ON SILICA GEL [0.03%]
N-碘代丁二酰亚胺和HF-BF4-硅胶催化下硫糖氨衍生物与伯醇的温和且选择性的O-苷化反应
Michio Kurosu,Kai Li
Michio Kurosu
Selective glycosylations of primary alcohols with the thioglucosaminide 1 are achieved by using NIS and HBF(4)-SiO(2). HBF(4)-SiO(2) is a mild Brønsted acid which requires primary alcohols or phenols to effectively activate 1 with NIS at r...
APPLICATIONS OF MULTICOMPONENT ASSEMBLY PROCESSES TO THE FACILE SYNTHESES OF DIVERSELY FUNCTIONALIZED NITROGEN HETEROCYCLES [0.03%]
用于合成多种功能化氮杂环的多组分缩合反应及其应用
James R Donald,Brett A Granger,Simon Hardy et al.
James R Donald et al.
Several multicomponent assembly processes have been developed for the synthesis of intermediates that may be elaborated by a variety of cyclizations to generate a diverse array of highly functionalized heterocycles from readily-available st...
CATALYTIC DYNAMIC RESOLUTION APPLIED TO THE SYNTHESIS OF 2,6-DISUBSTITUTED PIPERIDINES: PREPARATION OF (+)-LUPETIDINE AND (-)-EPIDIHYDROPINIDINE [0.03%]
催化动态动力学 resolutions合成2,6-双取代的哌啶：(+)-lupetidine和(-)-epidehydropinidine的制备
Timothy K Beng,Robert E Gawley
Timothy K Beng
The diastereoselective synthesis of trans-2,6-disubstituted piperidines has been rendered enantioselective by incorporating a catalytic dynamic resolution into the first alkylation step. The method has been applied to the synthesis of (-)-e...
UTILIZTION OF THE SUZUKI COUPLING TO ENHANCE THE ANTITUBERCULOSIS ACTIVITY OF ARYL OXAZOLES [0.03%]
利用铃木偶联反应增强芳基噁唑的抗结核活性
Garrett C Moraski,Scott G Franzblau,Marvin J Miller
Garrett C Moraski
Potent antituberculosis aryl oxazoles can be made in an efficient three step process--formation of β-hydroxy amides with serine benzyl ester; cyclization to afford oxazolines; and then dehydration to give the corresponding oxazoles. Furthe...
STUDIES ON THE BIOSYNTHESIS OF THE STEPHACIDINS AND NOTOAMIDES. TOTAL SYNTHESIS OF NOTOAMIDE S [0.03%]
诺妥amide S的全合成及链格孢酸和诺妥胺生物合成途径的研究
Timothy J McAfoos,Shengying Li,Sachiko Tsukamoto et al.
Timothy J McAfoos et al.
Notoamide S has been suggested to be the final common precursor between two different Aspergillus sp. fungal strains before diverging to form enantiomerically opposite natural products (+)- and (-)-stephacidin A and (+)- and (-)-notoamide B...
Feasible Synthesis of Antagonist of GPR40 by Constructing 2-Thiouracil Ring viaAcid Mediated Cyclization [0.03%]
酸介导环化构建2-硫脲嘧啶环合成GPR40拮抗剂的可行性研究
Yongfeng Zhao,Yang Song,Xiulin Shen et al.
Yongfeng Zhao et al.
GW1100 is an antagonist of GPR40 identified by high throughput screening recently. The synthesis of GW1100 has been developed. The key step involves cyclization of the 2-thiouracil heterocycle under acidic condition at room temperature.
Synthesis of Human Cancer Associated Globo-H (MBr1) Glycosylamino Acid: Some Mechanistic and Conformational Reinvestigations [0.03%]
人癌关联糖脂Globo-H(Mbr1)糖氨酰胺酸合成及若干合成和构象的再研究
Jianglong Zhu,Qian Wan,Guangbin Yang et al.
Jianglong Zhu et al.
The synthesis of an extended globo-H (MBr1 antigen) in the form of a glycosylamino acid is reported. By careful NMR analysis, we found an interesting conformational "flip" on the E ring of some synthetic intermediates. An explanation offere...
EXPLORATION OF BRAVERMAN REACTION CHEMISTRY. SYNTHESIS OF TRICYCLIC DIHYDROTHIOPHENE DIOXIDE DERIVATIVES FROM BISPROPARGYL SULFONES [0.03%]
布拉弗曼反应化学研究。从双丙炔基硫代烷合成三环化二氢噻吩二氧化物衍生物
Ken S Feldman,Brandon R Selfridge
Ken S Feldman
The base-mediated bicyclization of unsymmetrical bispropargyl sulfones furnishes varying yields of dihydroisobenzothiophene dioxides through a presumed diradical intermediate. Attempts to trap a putative thiophene dioxide intermediate via D...
ASYMMETRIC SYNTHESIS OF THE ABCD RING SYSTEM OF DAPHNILACTONE B VIA A TANDEM, DOUBLE INTRAMOLECULAR, [4+2]/[3+2] CYCLOADDITION STRATEGY [0.03%]
串联双分子[4+2]/[3+2]环加成策略非对称合成喜树碱并环系统ABCD_ring_system_of_daphnilactone_B_via_a_tandem_double_intramolecular_cycloaddition_strategy
Scott E Denmark,Son T Nguyen,Ramil Y Baiazitov
Scott E Denmark
An asymmetric synthesis of the ABCD ring system of daphnilactone B is described. The synthesis features a tandem, double intramolecular, [4+2]/[3+2] cycloaddition of a highly functionalized, enantiomerically enriched nitroalkene to generate...