AbstractHerein, we report a conceptually new, general, and efficient approach for the synthesis of valuable ortho‐azido‐1,5‐disubstituted tetrazole and one‐pot synthesis of ortho‐triazoletetrazole derivatives mainly via PIDA mediated N−N cleavage of the azole ring of 2H‐indazoles using TMSN3. This current methodology represents an array of unsymmetrical ortho‐azidotetrazole and ortho‐triazoletetrazole derivatives with wide functional group tolerance in good to excellent yields under mild reaction conditions. The practical utility of this reaction was showcased through successful scale‐up synthesis and a variety of subsequent derivatizations of ortho‐azidotetrazole products. Mechanistic investigations indicate that the reaction proceeds through a radical pathway.

01 Feb 2025·Current Organic Chemistry

Synthesis of Pregna-1,4,16-triene-3,20-dione from a Mixture of Soybean Phytosterols using a Combination of Chemical and Microbiological Methods

Author: Savinova, Tatiana Stepanovna ; Huy, Luu Duc ; Kazantsev, Alexey Vitalievich ; Donova, Marina Viktorovna ; Fokina, Victoria Valerievna

:In this paper, we present an efficient procedure for the transformation of a soybean phytosterol mixture into pregna-1,4,16-triene-3,20-dione, which is a key intermediate for the synthesis of valuable corticoids. The possibility of using two alternative methods for 1(2)-dehydrogenation of pregna-4,16-diene-3,20-dione - chemical and microbiological - was shown. Microbiological 3-keto-4-ene steroid 1(2)-dehydrogenation was carried out using actinobacterial cells of Nocardioides simplex VKM Ac-2033D. The structures of the synthesized compounds were confirmed by the IR, MS, and 1H-NMR methods.

01 Feb 2025·Journal of Molecular Structure

Reshaping the aggregation landscape of benzothiadiazole employing steroidal scaffolds and conformationally free alkyne tethers

Author: Maldonado-Dominguez, Mauricio ; Romero-Avila, Margarita ; Carreón-Castro, María del Pilar ; Carreon-Castro, Maria del Pilar ; Maldonado-Domínguez, Mauricio ; Alvarez-Venicio, Violeta ; Romero-Ávila, Margarita ; Ruiz-Deance, Sofía ; Arcos-Ramos, Rafael ; Ruiz-Deance, Sofia

In this study, we target the introduction of conformational freedom to BTD, aiming to unlock new solid-state arrangements that were previously inaccessible, while striving to maintain its high fluorescence quantum yield.Our approach is grounded in a detailed exploration of the conformational space of designed mols., employing mol. mechanics to predict and evaluate the impact of structural modifications on solubility and solid-state behavior.By strategically flanking the BTD core with steroidal fragments through alkyne bridges, we not only introduce bulky elements that disrupt the native crystal-packing landscape of pristine BTD, but also ensure significant rotational freedom around the carbon-carbon triple bonds.This design strategy allows the mols. to explore a wide range of conformations, potentially facilitating the formation of novel solid-state supramol. arrangements.The synthesis of these compounds revealed that they exhibit adequate processability in solution and form solids that prove crystalline by powder X-ray diffraction, but do not readily form macroscopic crystals as BTD normally does.The steroid fragments play a crucial role in determining the supramol. organization of these compoundsDepending on the specific functional groups present on the steroid skeleton, primary interactions such as hydrogen bonding and secondary interactions related to facial amphiphilicity dictate the overall arrangement of mols. in the solid state.Remarkably, the modifications successfully preserve the intrinsic high fluorescence quantum yield of the BTD core.This achievement underscores the potential of incorporating conformational flexibility into mol. design to access new material properties while retaining desirable photophys. characteristics.

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Amenorrhea	China	Qinhuangdao Zizhu Pharmaceutical Co. Ltd.	-
Dysmenorrhea	China	Qinhuangdao Zizhu Pharmaceutical Co. Ltd.	-
Uterine Hemorrhage	China	Qinhuangdao Zizhu Pharmaceutical Co. Ltd.	-

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