Category: piperidines. Authors Wu, J; Zheng, CM; Li, BY; Hawkins, JM; Scott, SL in ROYAL SOC CHEMISTRY published article about in [Wu, Jing; Zheng, Chunming; Scott, Susannah L.] Univ Calif Santa Barbara, Dept Chem Engn, Santa Barbara, CA 93106 USA; [Li, Bryan] Pfizer Global Res & Dev, Chem R&D La Jolla Lab, San Diego, CA 92121 USA; [Hawkins, Joel M.] Pfizer Global Res & Dev, Groton, CT 06371 USA; [Scott, Susannah L.] Univ Calif Santa Barbara, Dept Chem & Biochem, Santa Barbara, CA 93106 USA in 2021, Cited 64. The Name is 1,4-Dioxa-8-azaspiro[4.5]decane. Through research, I have a further understanding and discovery of 177-11-7
N-Boc deprotection (deBoc) is a common reaction in pharmaceutical research and development, as well as pharma manufacturing. Use of a catalyst lowers the required reaction temperature, and heterogeneous catalysts allow the reaction to be conducted in a continuous flow reactor with a low-boiling solvent, facilitating product separation and enhancing efficiency and productivity relative to a batch process. In this study, we explore the use of simple solid Bronsted acid catalysts to achieve continuous N-Boc deprotection of amines, without additional workup steps. Using THF as the solvent, H-BEA zeolite affords high yields of a variety of aromatic and aliphatic amines, often in residence times of less than a minute at 140 degrees C. The same catalyst/solvent combination is ineffective in batch conditions, due to the much lower temperature of refluxing THF. Boc-protected p-chloroaniline was deprotected with a throughput of 18 mmol p-chloroaniline per h per g(cat), sustained over 9 h. The active sites of the zeolite do not appear to be directly associated with the Al framework substitution in the micropores, since partially ion-exchanged Na/H-BEA shows activity similar to H-BEA. The strong Bronsted acid sites (framework [Si(OH)Al]), are likely poisoned by the amine product. Moderate Bronsted acid sites associated with silanol defects near Al on or near the external surface (and not susceptible to Na+-exchange) are presumably the active sites, since they are not poisoned even by more basic aliphatic amines.
Category: piperidines. About 1,4-Dioxa-8-azaspiro[4.5]decane, If you have any questions, you can contact Wu, J; Zheng, CM; Li, BY; Hawkins, JM; Scott, SL or concate me.
Reference：
Piperidine – Wikipedia,
Piperidine | C5H7510N – PubChem