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| 1 | The effect of umbrella-type branching on the blood circulation and tumor targeting of star-branched PLA-PMPC copolymer micelles显示文摘The effect of branching on the blood circulation and tumor targeting of polymer nanovehicles in vivo was investigated in this study. For the purpose, star-branched poly(lactic acid) and poly(2-methacryloyloxyethyl phosphorylcholine)(PLA-PMPC)copolymers with umbrella-type AB3,(AB3)_(2), and(AB3)_(3) architecture were synthesized by branching at the PLA core. Micelles self-assembled from these copolymers were used to evaluate the effect of core branching on blood circulation and tumor targeting. The results showed that branching changed the behavior of polymeric self-assembly in solution, thereby changing the size and surface anti-fouling performance of the polymeric micelles. Moreover, star-branched copolymer micelles with a higher branching degree allowed their payload to persist better in blood(half-time prolonged from 7.1, 8.6 to 13.8 h) and for a 1.72-fold higher content at the tumor site. These studies suggest that raising the branching degree of amphiphilic copolymer potentially offers a promising strategy for the design of carriers capable of enhanced circulation and targeting in vivo. | LONG LiXia CHENG LinJie HOU JingJing WANG LiMei WANG Xu HE LiGang LI SiDi ZHAO Jin HOU Xin KANG ChunSheng YUAN XuBo | 2021 | Science China(Technological Sciences)2021，64，1： | 0 |
| 2 | Palladium-catalyzed tandem Heck/carbonylation/ aminocarbonylation en route to chiral heterocyclic α-ketoamides显示文摘An unprecedented tandem carbonylation/aminocarbonylation triggered by palladium-catalyzed enantio-selective Heck-type exocyclopalladation delivering chiral heterocyclicα-ketoamides has been developed.The uncommon double CO insertion into theσ-alkylpalladium intermediate takes place selectively under atmospheric pressure of CO using alkylamine as the nucleophile.Unique structures hybridizing alkylα-ketoamides with indolin-2-one containing a C3 all-carbon quaternary stereogenic center and 5,7-dihydro-6H-dibenzo[b,d]azepin-6-one containing a thermodynamically stabilized stereogenic biaryl axis are produced in good yields with excellent enantio-and/or diastereoselectivities. | Huaanzi Hu Ting Yu Sidi Cheng Jing Li Chunfang Gan Shuang Luo Qiang Zhu | 2022 | Organic Chemistry Frontiers2022，9，4： | 0 |
| 3 | A New Saddle-Shaped Aza Analog of Tetraphenylene: Atroposelective Synthesis and Application as a Chiral Acylating Reagent显示文摘(Z)-7-Aryl-5-acyldibenzo[e,g][1,4]diazocin-6(5H)-one,a unique saddle-shaped bridged biaryl containing synchronized aryl–aryl and N-aryl stereogenic axes,was constructed for the first time in good yields with up to 96%enantiomeric excess(ee).The threecomponent coupling reaction,involving aryl iodide,2,2′-diisocyano-1,1′-biphenyl,and carboxylate,constructs the eight-membered ring in an atroposelective manner through palladium-catalyzed double isocyanide insertion followed by C–Obond formation during reductive elimination and amide formation after acyl transfer. | Yu Luo Sidi Cheng Yan Peng Xilong Wang Jing Li Chunfang Gan Shuang Luo Qiang Zhu | 2022 | CCS Chemistry2022，4，9： | 0 |
| 4 | Inherently Chiral 6,7-Diphenyldibenzo [e,g][1,4]diazocine: Enantioselective Synthesis and Application as a Ligand Platform显示文摘Inherently chiral 6,7-diphenyldibenzo[e,g][1,4]diazocine(DDD)has been synthesized enantioselectively for the first time via chiral phosphoric acid(CPA)-catalyzed cyclocondensation of readily available[1,1′-biphenyl]-2,2′-diamine(1a)and benzil(2a)in 82%yield,with 98%ee under mild reaction conditions.The strategy could also be applied to racemic biaryl diamines through kinetic resolution.The unexpectedly high interconversion energy barriers between the enantiomers(ΔG=39.5 kcal/mol)and the chemical stability rendered DDD an ideal platform for developing new chiral ligands and catalysts.Unique inherently chiralDDD-based phosphoramidites,phosphoric acid,mono-and diphosphine ligands were prepared from optically pure diphenol derivative DDDOL as a common precursor.Preliminary asymmetric reactions catalyzed by Pd or Rh in the presence of newly developed ligands exhibited comparable or even better enantioselectivities than the corresponding BINOLor SPINOL-derived ligands.Density functional theory calculation revealed the origin of the enantioselectivity during the process. | Yu Luo Xilong Wang Weiming Hu Yan Peng Chaoqin Wang Ting Yu Sidi Cheng Jing Li Yimiao He Chunfang Gan Shuang Luo Qiang Zhu | 2023 | CCS Chemistry2023，5，4： | 0 |
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