218900-56-2Relevant articles and documents
Group-assisted Purification (GAP) Chemistry/Technology in synthesizing the chiral intermediate of rivastigmine and its ?-Alkyl benzylamine analogues
Yang, Bing,Zhang, Chun-Yan,Xu, Jing,Zheng, Da-Jun,Wang, Xiao-Ying,Dai, Hong,Shi, Yu-Jun,Zhu, Hai-Liang
, p. 1065 - 1068 (2019/08/21)
Introduction of (S)-configuration is the key step in the synthesis of the anti-dementia drug Rivastigmine. Twenty-one alkylation products were obtained through simple washing with hexane/ethyl acetate (v/v: 10/1) in good yields (>85%) and high diastereoselectivity (up to >99:1 dr). Moreover, the chiral auxiliary could be easily dissociated and readily regenerated. That is, the synthesis was proved to follow group-assisted purification (GAP) chemistry/technology. In addition, the chiral amine produced by this asymmetric alkylation reaction was effectively used in the synthesis of Rivastigmine.
NOVEL N-PYRAZINIL-PHENYLSULFONAMIDE DERIVATIVES AS CHEMOKINE RECEPTOR MODULATORS FOR USE IN THE TREATMENT OF ASTHMA
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Page/Page column 32-33, (2010/11/26)
The invention provides a compound of formula (I), wherein R1, R2 and R3 are as defined in the specification, pharmaceutical compositions containing them, a process for preparing the pharmaceutical compositions, and their use in therapy.