Higher Responder Rates Observed With Live Participant Assessment Versus Photographic Assessment After VYC-20L Hyaluronic Acid Treatment for Chin Augmentation.

BACKGROUND: In an evaluator-blinded, randomized controlled trial, the hyaluronic acid soft-tissue filler VYC-20L injectable gel was safe and effective for correcting volume deficits and retrusion in the chin. OBJECTIVES: The objective of this subanalysis was to compare responder rates obtained with photographic vs live assessments. METHODS: Participants were randomized 3:1 to VYC-20L treatment or a 6-month, no-treatment control period followed by optional treatment. Responder rates (≥1-point improvement from baseline on the validated Allergan Chin Retrusion Scale [ACRS]) obtained with photographic assessments and live assessments at Month 6 were compared. Prespecified subgroup analyses compared responder rates by baseline ACRS severity, filler volume, cannula usage, and investigation site. RESULTS: VYC-20L was effective for chin augmentation as evaluated with both live and photographic assessments. The ACRS responder rates at Month 6 were 91.8% with live assessments and 56.3% with photographic assessments. Consistently higher response rates were observed by live vs photographic assessment regardless of baseline ACRS severity, filler volume, cannula usage, and investigation site. CONCLUSIONS: Live assessment of ACRS response after VYC-20L treatment resulted in higher responder rates than photographic assessment, supporting the use of live assessment for this indication to approximate real-world clinical practice.

Boc-SPPS: Compatible Linker for the Synthesis of Peptide o-Aminoanilides.

A protection strategy is described for the efficient synthesis of peptide o-aminoanilides using in situ neutralization protocols for Boc-SPPS. On-resin protection of Boc-protected aminoacyl o-aminoanilides is achieved with 2-chlorobenzyl chloroformate. Activation through a peptidyl-benzotriazole intermediate allows for facile conversion to peptide-thioesters for use in native chemical ligation. In addition to providing a robust alternative to established thioester resins, as a latent thioester, the peptide o-aminoanilide has broad utility in convergent ligation strategies.

Synthesis of benzannulated heterocycles by twofold Suzuki-Miyaura couplings of cyclic diarylborinic acids.

Two-fold Suzuki-Miyaura cross-couplings of cyclic diarylborinic acids are described. This novel annulation method enables the synthesis of benzo-fused heterocycles from dihaloarenes or gem-dibromoolefins.

Halogen bonding between anions and iodoperfluoroorganics: solution-phase thermodynamics and multidentate-receptor design.

The interactions of iodoperfluoroarenes and -alkanes with anions in organic solvent were studied. The data indicates that favorable halogen-bonding interactions exist between halide anions and the monodentate model compounds C(6)F(5)I and C(8)F(17)I. These data served as a basis for the development of preorganized multidentate receptors capable of high-affinity anion recognition. Several new receptor architectures were prepared, and the multidentate-iodoperfluorobenzoate-ester design, as described in a preliminary communication, was evaluated in more detail. Computation was employed to better interpret the structure-activity relationships arising from these studies. Investigations of the thermodynamics of anion binding (by van't Hoff analysis) and solvent effects reveal details of these halogen bonding interactions.

Measurements of weak halogen bond donor abilities with tridentate anion receptors.

The chelate effect of a tridentate receptor is exploited to determine halogen bonding association constants that vary by several orders of magnitude, including interactions of weak donors for which thermodynamic data were not previously available. Free energy relationships with computed and experimental properties hold over this wide range of donors. The strengths of iodine- and bromine-based halogen bonds, CH-anion and anion-arene interactions are compared.

Palladium-catalyzed C-H bond functionalization with arylsulfonyl chlorides.

Selective C-H bond functionalization enables efficient access to valuable products from relatively simple precursors and thus remains a longstanding challenge in organic synthesis. This communication highlights the discovery of arylsulfonyl chlorides as readily available, inexpensive, and versatile reagents for C-H bond functionalization. A novel Pd-catalyzed synthesis of arylsulfones that features a rare C-H bond activation/functionalization to form a C-S bond is presented. By simple alterations of the reaction parameters, Pd-catalyzed C-Cl and C-C bond formation can also be achieved using arylsulfonyl chlorides as the oxidant.

Intermolecular cope-type hydroamination of alkenes and alkynes using hydroxylamines.

The development of the Cope-type hydroamination as a method for the metal- and acid-free intermolecular hydroamination of hydroxylamines with alkenes and alkynes is described. Aqueous hydroxylamine reacts efficiently with alkynes in a Markovnikov fashion to give oximes and with strained alkenes to give N-alkylhydroxylamines, while unstrained alkenes are more challenging. N-Alkylhydroxylamines also display similar reactivity with strained alkenes and give modest to good yields with vinylarenes. Electron-rich vinylarenes lead to branched products while electron-deficient vinylarenes give linear products. A beneficial additive effect is observed with sodium cyanoborohydride, the extent of which is dependent on the structure of the hydroxylamine. The reaction conditions are found to be compatible with common protecting groups, free OH and NH bonds, as well as bromoarenes. Both experimental and theoretical results suggest the proton transfer step of the N-oxide intermediate is of vital importance in the intermolecular reactions of alkenes. Details are disclosed concerning optimization, reaction scope, limitations, and theoretical analysis by DFT, which includes a detailed molecular orbital description for the concerted hydroamination process and an exhaustive set of calculated potential energy surfaces for the reactions of various alkenes, alkynes, and hydroxylamines.