Weiping Tang

Bio: Weiping Tang is an academic researcher from University of Wisconsin-Madison. The author has contributed to research in topics: Cycloaddition & Medicine. The author has an hindex of 42, co-authored 187 publications receiving 5450 citations. Previous affiliations of Weiping Tang include Broad Institute & Howard Hughes Medical Institute.

Enantioselective bromolactonization of conjugated (Z)-enynes.

Abstract: A catalytic enantioselective syn-1,4-bromolactonization of conjugated (Z)-enynes was reported. Diastereomeric ratios >20:1 and up to 99% enantiomeric excesses were observed. Di-, tri-, and tetra-substituted bromoallenes were prepared together with lactone heterocycles efficiently and stereoselectively. Preliminary investigations suggest that the chiral catalyst may serve as a bifunctional reagent by interacting with both a carboxylic acid nucleophile and NBS electrophile.

Use of a regional, relict landscape to measure vertical deformation of the eastern Tibetan Plateau

Abstract: [1] Field work and topography analysis show that remnant, local areas of a low-relief landscape or erosion surfaces are geographically continuous across the southeastern Tibetan Plateau margin. We correlate these remnant surfaces as a paleolandscape that formed at low elevation. Remnants of this paleolandscape are preserved because incision of the fluvial system has been largely limited to major rivers and principal tributaries and has not yet progressed throughout the entire fluvial network. The incomplete adjustment of the fluvial system signals initiation of rapid bedrock incision into a developing plateau margin, and erosional denudation is concentrated in the major river channels. This interpretation contradicts earlier notions that low-gradient, regional topography is the product of regional elevation reduction by intense landscape dissection due to the presence of several large southeast flowing rivers. The modern altitude of the reconstructed paleolandscape (or “relict landscape”) constrains the vertical displacement of the plateau surface in response to crustal thickening and subsequent erosion during the lateral growth of the Tibetan Plateau. Regional preservation of the relict landscape is consistent with minor surface disruption by late Cenozoic thrust faults and folds and supports a model of distributed lower crustal thickening. Because significant erosion is limited to narrow river gorges, an increase in the plateau elevation due to isostatic rebound is minor. Therefore we propose that the modern elevation of the relict landscape reflects isostatically compensated thickening of the lower crust.

Divergent Enantioselective Synthesis of (−)-Galanthamine and (−)-Morphine

Abstract: An efficient divergent synthetic strategy for the synthesis of the opiate and amaryllidaceae alkaloids emerges by employing a Pd-catalyzed asymmetric allylic alkylation (AAA) to set the stereochemistry. Three generations of syntheses of galanthamine are discussed in detail with particular focus on the scope of the palladium-catalyzed AAA reactions and intramolecular Heck reactions. The pivotal tricyclic intermediate is available in six steps from 2-bromovanillin and the monoester of methyl 6-hydroxycyclohexene-1-carboxylate. This intermediate requires only two steps to convert to (-)-galanthamine. Using a Heck vinylation, we found that the fourth ring of codeine/morphine could be formed. The final ring formation involves a novel visible light-promoted hydroamination. Thus, six steps are required to convert the pivotal tricyclic intermediate into codeine, which has been demethylated in high yield to morphine.

Neuroendocrine Tumor-Targeted Upconversion Nanoparticle-Based Micelles for Simultaneous NIR-Controlled Combination Chemotherapy and Photodynamic Therapy, and Fluorescence Imaging.

Abstract: Although neuroendocrine tumors (NETs) are slow growing, they are frequently metastatic at the time of discovery and no longer amenable to curative surgery, emphasizing the need for the development of other treatments. In this study, multifunctional upconversion nanoparticle (UCNP)-based theranostic micelles are developed for NET-targeted and near-infrared (NIR)-controlled combination chemotherapy and photodynamic therapy (PDT), and bioimaging. The theranostic micelle is formed by individual UCNP functionalized with light-sensitive amphiphilic block copolymers poly(4,5-dimethoxy-2-nitrobenzyl methacrylate)-polyethylene glycol (PNBMA-PEG) and Rose Bengal (RB) photosensitizers. A hydrophobic anticancer drug, AB3, is loaded into the micelles. The NIR-activated UCNPs emit multiple luminescence bands, including UV, 540 nm, and 650 nm. The UV peaks overlap with the absorption peak of photocleavable hydrophobic PNBMA segments, triggering a rapid drug release due to the NIR-induced hydrophobic-to-hydrophilic transition of the micelle core and thus enabling NIR-controlled chemotherapy. RB molecules are activated via luminescence resonance energy transfer to generate 1O2 for NIR-induced PDT. Meanwhile, the 650 nm emission allows for efficient fluorescence imaging. KE108, a true pansomatostatin nonapeptide, as an NET-targeting ligand, drastically increases the tumoral uptake of the micelles. Intravenously injected AB3-loaded UCNP-based micelles conjugated with RB and KE108-enabling NET-targeted combination chemotherapy and PDT-induce the best antitumor efficacy.

C-H bond functionalization: emerging synthetic tools for natural products and pharmaceuticals

Abstract: The direct functionalization of C-H bonds in organic compounds has recently emerged as a powerful and ideal method for the formation of carbon-carbon and carbon-heteroatom bonds. This Review provides an overview of C-H bond functionalization strategies for the rapid synthesis of biologically active compounds such as natural products and pharmaceutical targets.

Asymmetric transition-metal-catalyzed allylic alkylations: applications in total synthesis.

Abstract: A. Primary Alcohols as Nucleophiles 2931 B. Carboxylates as Nucleophiles 2931 C. Alkylations with Phenols 2932 IV. Nitrogen Nucleophiles in AAA Total Synthesis 2935 A. Alkylamines as Nucleophiles 2935 B. Azides as a Nucleophile 2936 C. Sulfonamide Nucleophiles 2937 D. Imide Nucleophiles 2938 E. Heterocyclic Amine Nucleophiles 2940 V. Sulfur Nucleophiles 2941 VI. Summary and Conclusions 2941 VII. Acknowledgment 2941 VIII. References 2942 I. Considerations for Enantioselective Allylic Alkylation

Hydroamination: direct addition of amines to alkenes and alkynes.

Abstract: 8.4.5. Nitromercuration Reactions 3878 9. Hydroamination of Alkenes and Alkynes under Microwave Irradiation 3878 * To whom correspondence should be addressed. Phone: +49 241 8

Robust cardiomyocyte differentiation from human pluripotent stem cells via temporal modulation of canonical Wnt signaling

Abstract: Human pluripotent stem cells (hPSCs) offer the potential to generate large numbers of functional cardiomyocytes from clonal and patient-specific cell sources. Here we show that temporal modulation of Wnt signaling is both essential and sufficient for efficient cardiac induction in hPSCs under defined, growth factor-free conditions. shRNA knockdown of β-catenin during the initial stage of hPSC differentiation fully blocked cardiomyocyte specification, whereas glycogen synthase kinase 3 inhibition at this point enhanced cardiomyocyte generation. Furthermore, sequential treatment of hPSCs with glycogen synthase kinase 3 inhibitors followed by inducible expression of β-catenin shRNA or chemical inhibitors of Wnt signaling produced a high yield of virtually (up to 98%) pure functional human cardiomyocytes from multiple hPSC lines. The robust ability to generate functional cardiomyocytes under defined, growth factor-free conditions solely by genetic or chemically mediated manipulation of a single developmental pathway should facilitate scalable production of cardiac cells suitable for research and regenerative applications.

The Geological Evolution of the Tibetan Plateau

Abstract: The geological evolution of the Tibetan plateau is best viewed in a context broader than the India-Eurasia collision zone. After collision about 50 million years ago, crust was shortened in western and central Tibet, while large fragments of lithosphere moved from the collision zone toward areas of trench rollback in the western Pacific and Indonesia. Cessation of rapid Pacific trench migration (∼15 to 20 million years ago) coincided with a slowing of fragment extrusion beyond the plateau and probably contributed to the onset of rapid surface uplift and crustal thickening in eastern Tibet. The latter appear to result from rapid eastward flow of the deep crust, probably within crustal channels imaged seismically beneath eastern Tibet. These events mark a transition to the modern structural system that currently accommodates deformation within Tibet.