Visible-light-induced [3+2] cycloadditions of donor/donor diazo intermediates with alkenes to achieve (spiro)-pyrazolines and pyrazoles.

To date, [3 + 2] cycloadditions of diazo esters with alkynes or alkenes have been a robust tool to generate pyrazoles and pyrazolines. However, methods capable of generating donor/donor diazo species from readily available N-tosylhydrazones to furnish [3 + 2] cycloadditions, remain elusive. Herein, we describe the first visible-light-induced [3 + 2] cycloadditions of donor/donor diazo precursors with alkenes to afford pyrazoles and novel (spiro)pyrazolines bearing a quaternary center. This protocol shows a tolerable substrate scope covering versatile carbonyl compounds and alkenes. Late-stage functionalization of bioactive molecules, one-pot approach, and gram-scale synthesis have also been introduced successfully to prove the practicability. At last, mechanistic experiments and DFT studies suggested the formation of non-covalent interactions enabling the activation of N-tosylhydrazones and the formation of the donor/donor diazo intermediates.

Ultrasonographic evaluation of the change in uterine fibroids induced by treatment with a GnRH analog.

OBJECTIVE: To investigate the change in volume of uterine fibroids after GnRH analog (GnRHa) treatment. MATERIALS AND METHODS: Twenty-five patients who had a uterine leiomyoma were included in this study. Four of them were lost to follow-up during the study, and a myomectomy was performed on the remaining subjects. All of these patients received two doses, 4 weeks apart, each of 3.75 mg leuprorelin acetate subcutaneously (Leuplin depot, a GnRHa) before the operation. The vascularization index (VI), flow index (FI), vascularization-flow index (VFI), pulsative index (PI), resistance index (RI), vascular patterns (histogram), blood flows, and sizes (volume and largest diameter) of each fibroid were measured with power Doppler by the same technician every month before the operation. In addition, the total blood loss and time required for each operation were also recorded. RESULTS: Results of this study showed that the volume of the uterus and the fibroids, but not the vascularity, including VI, FI, VFI, PI and RI, decreased significantly after two doses of GnRHa treatment. In addition, blood loss during the operation decreased significantly compared to an untreated group. CONCLUSION: We found that the volumes of the uterus and fibroids decreased significantly after treatment with two consecutive doses (given a month apart) of GnRHa. The 3D color Doppler including a histogram and blood flow parameters is another useful tool for fibroid evaluation.