Original end-to-end smart diagnosis framework of systematic critical quality attributes meets FDA standards of phytomedicine by biosensor and multi-information fusion coupled with AI algorithm

Abstract

Great progress has been made in phytomedicine manufacturing based on the development of green chemistry. However, identifying critical variation sources and exploring interactive coupling mechanisms to ultimately feedback manufacturing remain...

Metal- and photocatalyst-free three-component strategy to prepare benzylalcohol-, aldehyde-substituted BCP building blocks

“…On the basis of our experimental observations and literature reports, we propose the mechanism shown in Scheme 2C. 15,18 Upon irradiation at 390-395 nm, ground-state benzaldehyde is excited to the singlet state, and subsequent intersystem crossing generates the more-reactive triplet state. Then ketyl and α-oxyalkyl form by means of hydrogen-atom transfer between the ether and the triplet state of the aldehyde.…”

“…Having investigated the mechanism, we next assessed the reaction's substrate scope (Scheme 3). A wide variety of aryl aldehydes with an electron-neutral, electron-donating, or electron-withdrawing substituent at the para position were reactive, delivering the desired products (4)(5)(6)(7)(8)(9)(10)(11)(12)(13)(14)(15)(16)(17)(18)(19) in good yields. In particular, various common functional groups were tolerated, such as halogen atoms (11, 12), a methanesulfonyl group (13), a ketone ( 14), an ester ( 17), a trifluoromethanesulfonyl group (18), and a pyrazole ring (19).…”

“…A wide variety of aryl aldehydes with an electron-neutral, electron-donating, or electron-withdrawing substituent at the para position were reactive, delivering the desired products (4)(5)(6)(7)(8)(9)(10)(11)(12)(13)(14)(15)(16)(17)(18)(19) in good yields. In particular, various common functional groups were tolerated, such as halogen atoms (11, 12), a methanesulfonyl group (13), a ketone ( 14), an ester ( 17), a trifluoromethanesulfonyl group (18), and a pyrazole ring (19). Intriguingly, several relatively sensitive yet versatile functional groups-cyano (15), boronic acid ester (16), formyl (20), and alkyne (21)-tolerated the difunctionalization conditions well, which shows the potential utility of this protocol for synthetic and medicinal chemistry applications.…”

“…Recently, we reported an environmentally friendly method for photoinduced generation of ketyl radicals from aromatic carbonyl compounds for the construction of C-C bonds without any external photocatalyst. 18 Because of the radical character of the triplet excited states of aryl aldehydes, they can abstract a hydrogen atom from an ether to generate ketyl and α-oxyalkyl radicals. 19 These two radicals could then trigger ring-opening of [1.1.1]propellane by means of a radical-coupling process, resulting in the introduction of both an alcohol and an ether to the BCP.…”