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Bicyclo[1.1.1]pentanes (BCP's) have been applied in medicinal chemistry as bioisosteres for phenyl groups. In pursuit of novel BCP analogs, we reported the first synthesis of 2,2‐difluorobicyclo[1.1.1]pentanes (BCP–F2) in 2019. Herein, we detail the extension of our effort in the synthesis of BCP‐F2 analogs. [ABSTRACT FROM AUTHOR]

This Minireview focuses on selected topics in the syntheses of bicyclo[1.1.1]pentane (BCP) analogues. A brief historical introduction was included. The content covers various synthetic routes of 1‐substituted and 1,3‐disubstituted BCPs. Selective examples of synthetically useful building blocks are summarized for each category for synthetic organic chemists' and medicinal chemists' reference. A compare‐and‐contrast analysis is also applied to evaluate these routes and to demonstrate the progress of strategic functional group transformations using modern organic methodologies. By systematically analyzing the synthetic strategies to access these strained molecules, we also hope that this Minireview will provide inspirations for future developments in this area. [ABSTRACT FROM AUTHOR]

Context: Primary aldosteronism represents an important and common cause of hypertension and is characterized by autonomous aldosterone secretion that results in severe hypertension and hypokalemia. Nonetheless, its manifestations are atypical in some cases, which renders its diagnosis difficult. Case Description: Presented in this report is a Chinese female patient with blood pressure in the high-normal range, and her parathyroid hormone was significantly elevated. Elevated plasma aldosterone concentration plus suppressed plasma rennin activity was suggestive of primary aldosteronism. 68Ga-pentixafor positron emission tomography/computed tomography revealed an aldosterone-producing adenoma, which was globally the second of its kind ever reported so far. Moreover, the tumor was located in an extremely rare area. Conclusions: Patients with primary aldosteronism may present with normal or high-normal blood pressure and a significantly elevated parathyroid hormone. 68Ga-pentixafor PET/CT is potentially a helpful tool for the non-invasive characterization of patients with primary aldosteronism. [ABSTRACT FROM AUTHOR]

Recent years have seen novel modalities emerge for the treatment of human diseases resulting in an increase in beyond rule of 5 (bRo5) chemical matter. As a result, synthetic innovations aiming to enable rapid access to complex bRo5 molecular entities have become increasingly valuable for medicinal chemists' toolkits. Herein, we report the general synthesis of a new class of noncanonical amino acids (ncAA) with a cyclopropyl backbone to achieve conformational constraint and bearing C( sp 3 )-rich benzene bioisosteres. We also demonstrate preliminary studies toward utilities of these ncAA as building blocks for medicinal chemistry research.

Described herein is our effort toward achieving the decarboxylative functionalization of 2,2-difluorobicyclo[1.1.1]pentane (BCP-F 2 ) building blocks. When compared with the nonfluorinated bicyclo[1.1.1]pentane (BCP) analogues, we discovered divergent reactivities. This is the first successful decarboxylative coupling of BCP-F 2 building blocks reported via the photoredox mechanism.

We report our efforts toward achieving C(sp 2 )-C(sp 3 ) coupling reactions with 2,2-difluorobicyclo[1.1.1]pentane (BCP-F 2 ) building blocks. By comparing the reactivities of matching pairs of bicyclo[1.1.1]pentane (BCP) and BCP-F 2 analogues, we discovered that the Barluenga coupling reaction was the only cross-coupling protocol that translated well between the two structural motifs in contrast to other reported protocols. In this chemistry, a BCP-F 2 bearing a tosylhydrazone functional group is cross-coupled with an arylboronic acid. These results further expanded the scope of BCP-F 2 building blocks for potential applications in organic chemistry as well as medicinal chemistry.

Context: Primary aldosteronism represents an important and common cause of hypertension and is characterized by autonomous aldosterone secretion that results in severe hypertension and hypokalemia. Nonetheless, its manifestations are atypical in some cases, which renders its diagnosis difficult. Case Description: Presented in this report is a Chinese female patient with blood pressure in the high-normal range, and her parathyroid hormone was significantly elevated. Elevated plasma aldosterone concentration plus suppressed plasma rennin activity was suggestive of primary aldosteronism. 68 Ga-pentixafor positron emission tomography/computed tomography revealed an aldosterone-producing adenoma, which was globally the second of its kind ever reported so far. Moreover, the tumor was located in an extremely rare area. Conclusions: Patients with primary aldosteronism may present with normal or high-normal blood pressure and a significantly elevated parathyroid hormone. 68 Ga-pentixafor PET/CT is potentially a helpful tool for the non-invasive characterization of patients with primary aldosteronism., (Copyright © 2019 Cui, Zhang, Ding, Wang, Ma, Wang, Chang, Sun, Huo and Tong.)

Ethyne is employed as coupling partner in copper-mediated cross-coupling reactions with N-tosylhydrazones and α-diazoacetate, leading to the development of a new synthetic method for terminal allenes. With this novel coupling method, the terminal allenes were obtained in good yields and with excellent functional group tolerance. Copper carbene migratory insertion is proposed as the key step in these transformations.