TBHP/Et3N-Promoted Chemoselective Formylation and Peroxidation of Pyrrolo[2,1-a]isoquinolines.

An efficient formylation of pyrrolo[2,1-a]isoquinoline derivatives has been reached by the use of TBHP (tBuOOH) and Et3N as the mediator. In this strategy, CHO and CDO can be readily incorporated into heteroarenes by the utilization of CHCl3 and CDCl3 as the carbonyl sources. Interestingly, a solvent-controlled chemoselectivity was observed. The use of PhCl as a solvent resulted in dearomatization and peroxidation of pyrrolo[2,1-a]isoquinolines, delivering functionalized peroxides in 53-64% yields.

Iron-Catalyzed Synthesis of Peroxylpyrrolo[2,1-a]isoquinolines through Oxidative Dearomatization.

A mild late-stage modification of pyrrolo[2,1-a]isoquinolines was established through iron-catalyzed oxidative dearomatization and peroxidation. Peroxylated pyrroloisoquinolines have been prepared readily with hydroperoxide in low to good yields (up to 72%) at room temperature. Interestingly, the treatment of fully aromatized pyrrolo[1,2-a]quinolines under the current reaction system resulted in the formation of ring-opening products.

Dual colorimetric and near-infrared fluorescence probe for Hg2+ detection and cell imaging.

Hg2+ in the environment endangers human health, and a convenient monitoring method is needed for the detection of Hg2+. In this study, we constructed a dual colorimetric near-infrared fluorescent probe (E)-2-(3-(3-(1,3-dithian-2-yl)-4-hydroxystyryl)-5,5-dimethylcyclohex-2-en-1-ylidene)malononitrile (YF-Hg), based on the malononitrile isophorone. YF-Hg can detect Hg2+ rapidly and sensitively, with fluorescence emission in the near-infrared region (659 nm) with an obvious color change from violet to red in the visible light range. In addition, the low toxicity and large Stokes shift (191 nm) of YF-Hg also suggest that it is a potential tool for live-cell fluorescence imaging.

The synthesis of pennogenin 3-O-ß-D-glucopyranosyl-(1 → 3)-[α-L-rhamnopyranosyl-(1 → 2)]-ß-D-glucopyranoside.

Pennogenin 3-O-ß-D-glucopyranosyl-(1 → 3)-[α-L-rhamnopyranosyl-(1 → 2)]-ß-D-glucopyranoside, a monodesmosidic saponin isolated from Paris polyphylla Smith var. yunnanensis with promised antitumor activities, was firstly synthesized from glucoside thiol via nine steps and with 27% overall yield.

Hourly oral misoprostol administration for terminating midtrimester pregnancies: a pilot study.

OBJECTIVE: This pilot study retrospectively evaluated the outcomes of medical induction of termination of midtrimester pregnancies with hourly oral misoprostol administration. MATERIALS AND METHODS: Sixteen women with living fetuses, who had undergone pregnancy termination at 12-25 weeks of gestational age, were reviewed. The method of induction was hourly oral administration of misoprostol, given at doses of 200 µg/hr for the first 12 hours and 400 µg/hr after 12 hours until delivery. Data including the induction-to-delivery interval and total dosage of misoprostol were recorded and analyzed. RESULTS: All 16 women successfully underwent vaginal termination within 36 hours. The median induction-to-delivery interval was 12.0 hours (range, 6.3-30.9 hours), with 13 women (81.3%) undergoing vaginal delivery within 24 hours. The median total dosage of misoprostol was 2,600 µg. The most common side effect was diarrhea, which was easily relieved by medication. CONCLUSION: Our preliminary results show that oral administration of misoprostol at hourly intervals is a promising method for terminating midtrimester pregnancies.