The invention provides compounds of formula (I)
wherein R
1
, R
3
, L
1
, L
2
, G
1
, G
2
, A and m are as defined in the specification and optical isomers, racemates and tautomers thereof, and pharmaceutically acceptable salts thereof; together with processes for their preparation, pharmaceutical compositions containing them and their use in therapy. The compounds are inhibitors of microsomal prostaglandin E synthase-1.
Palladium-Catalyzed Asymmetric 1,4-Addition of Diarylphosphines to α,β-Unsaturated Sulfonamides
作者:Fanhua Xiao、Wei-Liang Duan、Guo-Fa Dai、Yu-Chuan Song
DOI:10.1055/s-0036-1591593
日期:2018.9
Abstract A pincer palladium-catalyzedasymmetric 1,4-addition of diarylphosphines to α,β-unsaturated sulfonamides was realized for the synthesis of chiral sulfonamide phosphines with up to 98% ee under mild conditions. A pincer palladium-catalyzedasymmetric 1,4-addition of diarylphosphines to α,β-unsaturated sulfonamides was realized for the synthesis of chiral sulfonamide phosphines with up to 98%
Bis-(sulfonylamino) derivatives for use in therapy
申请人:Bylund Johan
公开号:US09145380B2
公开(公告)日:2015-09-29
The invention provides compounds of formula (I) wherein R1, R3, L1, L2, G1, G2, A and m are as defined in the specification and optical isomers, racemates and tautomers thereof, and pharmaceutically acceptable salts thereof; together with processes for their preparation, pharmaceutical compositions containing them and their use in therapy. The compounds are inhibitors of microsomal prostaglandin E synthase-1.
Bis-(Sulfonylamino) derivatives for use in therapy
申请人:Bylund Johan
公开号:US20100331321A1
公开(公告)日:2010-12-30
The invention provides compounds of formula (I) wherein R
1
,R
3
,L
1
,L
2
,G
1
,G
2
, A and m are as defined in the specification and optical isomers, racemates and tautomers thereof, and pharmaceutically acceptable salts thereof; together with processes for their preparation, pharmaceutical compositions containing them and their use in therapy. The compounds are inhibitors of microsomal prostaglandin E synthase-1.
addition of the carbanion, followed by cyclization–fragmentation of the four-membered ring intermediate. In the absence of base, electron-rich aldehydes follow an alternative pathway of the Knoevenagel condensation to provide unsaturated 1,1-disulfonyl fluorides. We demonstrate also trapping of elusive ethene-1,1-disulfonyl fluoride, CH2═C(SO2F)2, with 4-(dimethylamino)pyridine (DMAP) that forms zwitterionic