- Synthesis of (±)-amathaspiramide F and discovery of an unusual stereocontrolling element for the [2,3]-stevens rearrangement
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A formal total synthesis of (±)-amathaspiramide F through a tandem palladium-catalyzed allylic amination/[2,3]-Stevens rearrangement is reported. The unexpected diastereoselectivity of the [2,3]-Stevens rearrangement was controlled by the substitution pat
- Soheili, Arash,Tambar, Uttam K.
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- Discovery of S1P agonists with a dihydronaphthalene scaffold
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Structure-activity relationship of sphingosine-1-phosphate receptor agonists was examined. Cinnamyl derivative 1 was modified to improve S1P 1 agonistic activity as well as selectivity over S1P3 agonistic activity. Dihydronaphthalene derivative 10d was identified as a potent S1P1 receptor agonist with high selectivity against S1P3 and enhanced efficacy in lowering peripheral lymphocyte counts in mice.
- Kurata, Haruto,Kusumi, Kensuke,Otsuki, Kazuhiro,Suzuki, Ryo,Kurono, Masakuni,Takada, Yuka,Shioya, Hiroki,Komiya, Takaki,Mizuno, Hirotaka,Ono, Takeji,Hagiya, Hiroshi,Minami, Masashi,Nakade, Shinji,Habashita, Hiromu
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scheme or table
p. 3885 - 3889
(2011/08/06)
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- COMPOUND CAPABLE OF BINDING S1P RECEPTOR AND PHARMACEUTICAL USE THEREOF
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A compound having an ability to bind to an S1P receptor (particularly EDG-6, preferably EDG-1 and EDG-6), for example, the compound represented by formula (I) of the present invention, a salt thereof, a solvate thereof or a prodrug thereof is useful for prevention and/or treatment of rejection of transplantation, graft-versus-host disease, autoimmune disease, allergic disease and the like. wherein ring A is a cyclic group; ring B is a cyclic group which may have substituent(s); X is a spacer having 1 to 8 atoms in its main chain, etc.; Y is a spacer having 1 to 10 atoms in its main chain, etc.; n is 0 or 1, wherein when n is 0, m is 1 and R1 is a hydrogen atom or a substituent, and wherein when n is 1, m is 0 or an integer of 1 to 7 and R1 is a substituent, and wherein m is 2 or more, R1s are the same or different.
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