Journal of Medicinal Chemistry p. 11138 - 11147 (2016)
Update date:2022-09-26
Topics:
Yang, Michael G.
Xiao, Zili
Dhar, T. G. Murali
Xiao, Hai-Yun
Gilmore, John L.
Marcoux, David
Xie, Jenny H.
McIntyre, Kim W.
Taylor, Tracy L.
Borowski, Virna
Heimrich, Elizabeth
Li, Yu-Wen
Feng, Jianlin
Fernandes, Alda
Yang, Zheng
Balimane, Praveen
Marino, Anthony M.
Cornelius, Georgia
Warrack, Bethanne M.
Mathur, Arvind
Wu, Dauh-Rurng
Li, Peng
Gupta, Anuradha
Pragalathan, Bala
Shen, Ding Ren
Cvijic, Mary Ellen
Lehman-Mckeeman, Lois D.
Salter-Cid, Luisa
Barrish, Joel C.
Carter, Percy H.
Dyckman, Alaric J.
We describe a highly efficient route for the synthesis of 4a (BMS-986104). A key step in the synthesis is the asymmetric hydroboration of trisubstituted alkene 6. Particularly given the known difficulties involved in this type of transformation (6 → 7), the current methodology provides an efficient approach to prepare this class of compounds. In addition, we disclose the efficacy of 4a in a mouse EAE model, which is comparable to 4c (FTY720). Mechanistically, 4a exhibited excellent remyelinating effects on lysophosphatidylcholine (LPC) induced demyelination in a three-dimensional brain cell culture assay.
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