85275-45-2Relevant articles and documents
Sustainable Route Toward N-Boc Amines: AuCl3/CuI-Catalyzed N-tert-butyloxycarbonylation of Amines at Room Temperature
Cao, Yanwei,Huang, Yang,He, Lin
, (2021/12/22)
N-tert-butoxycarbonyl (N-Boc) amines are useful intermediates in synthetic/medicinal chemistry. Traditionally, they are prepared via an indirect phosgene route with poor atom economy. Herein, a step- and atom-economic synthesis of N-Boc amines from amines, t-butanol, and CO was reported at room temperature. Notably, this N-tert-butyloxycarbonylation procedure utilized ready-made substrates, commercially available AuCl3/CuI as catalysts, and O2 from air as the sole oxidant. This catalytic system provided unique selectivity for N-Boc amines in good yields. More significantly, gram-scale preparation of medicinally important N-Boc amine intermediates was successfully implement, which demonstrated a potential application prospect in industrial syntheses. Furthermore, this approach also showed good compatibility with tertiary and other useful alcohols. Investigations of the mechanisms revealed that gold catalyzed the reaction and copper acted as electron transfer mediator in the catalytic cycle.
PYRAZOLE DERIVATIVES AS H4 ANTAGONIST COMPOUNDS
-
Paragraph 37; 46; 47, (2020/05/21)
The disclosures herein relate to novel compounds of formula (1): and salts thereof, wherein A; X;n; R1 and R2 are defined herein, and their use in treating, preventing, ameliorating, controlling or reducing the risk of disorders associated with H4 receptors.
Preparation method of N-tert-butyloxycarbonyl-3-piperidone and derivative thereof
-
Paragraph 0065-0066; 0068-0070, (2020/07/21)
The invention discloses a preparation method of N-tert-butyloxycarbonyl-3-piperidone, and the method comprises the following step: oxidizing N-tert-butyloxycarbonyl-3-hydroxypiperidine by virtue of aNaDCC-TEMPO system so as to generate N-tert-butyloxycarbonyl-3-piperidone. The invention also discloses a method for preparing (S)-N-tert-butyloxycarbonyl-3-hydroxypiperidine through an oxidation reaction and a reduction reaction by virtue of the NaDCC-TEMPO system. The method has the advantages of simple operation steps, high conversion rate and high product purity.