Synthesis and activity of 2-methyl-3-aminopropiophenones as centrally acting muscle relaxants
摘要:
Some novel 2-methyl-3-aminopropiophenones were synthesized and their centrally acting muscle relaxant activities were evaluated for an inhibitory effect on the flexor reflex in rats. The structure-activity relationships are discussed. In this series, 2-methyl-3-pyrrolidino-1-(4-trifluoromethylphenyl)-propan-1-one (28) showed significant centrally acting muscle relaxant activity. In addition, the activities of each enantiomer (28-(S) and (R)) were studied along with their acute toxicities. Compound 28-(R) was found to exhibit more potent activity and weaker acute toxicity than 28-(S). Accordingly, compound 28-(R) (NK433) is under development as a novel centrally acting muscle relaxant.
A polyphenylene ether resin composition containing the following Components (A) to (D) according at the following formulation ratio.
(A) 50 to 99.5 parts by weight of a polyphenylene ether
(B) 0.1 to 50 parts by weight of a partially hydrogenated aromatic alkenyl compound-conjugated diene block copolymer having a hydroxy group
and based on 100 parts by weight of the above resin composition,
(C) 0 to 950 parts by weight of a thermoplastic resin
and
(D) 0 to 10 parts by weight of a phosphorous acid triester
Halogen-magnesium exchange of various aryl halides is achieved with a magnesium ate complex at low temperatures; Tributylmagnesate ((Bu3MgLi)-Bu-n) induces facile iodine-magnesium exchange at -78 degreesC. Dibutylisopropylmagnesate ((PrBu2MgLi)-Pr-i-Bu-n) is more reactive than (Bu3MgLi)-Bu-n, and this reagent accomplishes selective bromine-magnesium exchange at -78 degreesC. This procedure is utilized for the preparation of various polyfunctionalized arylmagnesium species. The exchange of alkenyl halides using this method proceeds with retention of configuration of the double bond.
TERMINALLY UNSATURATED MACROMOLECULAR MONOMERS OF POLYFORMALS AND COPOLYMERS THEREOF
申请人:The B.F. Goodrich Company
公开号:EP0357691A1
公开(公告)日:1990-03-14
EP0357691A4
申请人:——
公开号:EP0357691A4
公开(公告)日:1992-03-18
PEG-BASED MACROMONOMERS, CHEMICALLY INERT POLYMERS PREPARED THEREFROM AND THE USE OF THESE POLYMERS FOR ORGANIC SYNTHESIS AND ENZYME REACTIONS