155396-71-7Relevant articles and documents
Construction of N-Boc monofluoromethyl aryl sulfones via Mannich reaction of α-amido sulfones with trifluoromethyl α-fluorinated arylsulfonyl gem-diols
Fang, Xiang,Wang, Wang,Wu, Fanhong,Yang, Xueyan
, (2020)
A mild and efficient nucleophilic monofluoromethylation of α-amido sulfones with trifluoromethyl α-fluorinated arylsulfonyl gem-diols as new building blocks has been developed, which affords N-Boc monofluoromethyl aryl sulfones in good yields with appropriate 5:1 diastereomeric ratio.
Synthetic method of dapoxetine and intermediate thereof
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Paragraph 0085-0088; 0114-0117, (2020/03/09)
The invention discloses a synthetic method of dapoxetine and its intermediate, i.e., (S)-3-(tert-butyloxycarbonyl)amino-3-phenylpropanol as shown in a formula 5 which is described in the specification. The synthetic method of (S)-3-(tert-butyloxycarbonyl)amino-3-phenylpropanol is as shown in a synthesis route which is described in the specification, wherein a compound 3 and acetaldehyde are subjected to a Mannich reaction in an organic solvent under the action of a supramolecular catalyst constructed by a chiral catalyst and a polymer so as to obtain a compound 4, and the polymer is at least one selected from of the group consisting of PEG 200, PEG 400, PEG 600, MeOPEG 750, PEG 800, PEG 1000, PPG 800 and PPG 1000. The dapoxetine is synthesized from the (S)-3-(tert-butyloxycarbonyl)amino-3-phenylpropanol prepared by using the above method according to steps as shown in the synthesis route. The synthetic method of dapoxetine and the intermediate thereof has the characteristics of usage of cheap and easily available raw materials, high yield and low cost, and is more beneficial to industrial production.
Br?nsted Acid-Catalyzed Aza-Ferrier Reaction of N, O-Allenyl Acetals: Synthesis of β-Amino-α-methylene Aldehydes
Tayama, Eiji,Ishikawa, Yuki
supporting information, p. 9405 - 9414 (2020/08/14)
A Tf2NH-catalyzed aza-Ferrier reaction of N,O-allenyl acetals was reported. This protocol provided various types of β-amino-α-methylene aldehydes as the products. The N,O-allenyl acetal substrates were easily prepared by base-induced isomerization of N,O-propargyl acetals with Triton B. The N,O-propargyl acetals were prepared from the corresponding aldehydes or lactams. Further synthetic applications of the products were also described.