制备了一系列具有羧基羧基酰胺N-取代基的Nα-(芳基磺酰基)-L-精氨酸酰胺衍生物,并测试了它们作为凝血酶凝血活性的抑制剂。当在Nα-(芳基磺酰基)-L-精氨酸酰胺衍生物(例如Nα-(芳基磺酰基)-L-精氨酸-N-丁基)的酰胺氮旁的碳原子中引入羧基时,获得最具抑制性的化合物。 -,N-(甲氧基乙基)-或N-(四氢糠基)甘氨酸和4-烷基-1- [Nα-(芳基磺酰基)-L-精氨酰基] -2-哌啶甲酸,I50为1-3 X 10( -7)M.
DOI:
10.1021/jm00186a003
作为产物:
描述:
溴乙酸叔丁酯 、 正丁胺 以
甲基叔丁基醚 为溶剂,
反应 16.0h,
以so as to obtain the title compound (4.67 g, yield: 100%) in the form of a colorless oily substance的产率得到N-butylglycine tert-butyl ester
N.sup.2 -arylsulfonyl-l-argininamides and the pharmaceutically
申请人:Mitsubishi Chemical Industries Limited
公开号:US04097472A1
公开(公告)日:1978-06-27
N.sup.2 -arylsulfonyl-L-argininamides and the pharmaceutically acceptable salts thereof have been found to be effective as pharmaceutical agents for the inhibition and suppression of thrombosis in mammals.
N.sup.2 -arylsulfonyl-L-argininamides and the pharmaceutically
申请人:Mitsubishi Chemical Industries Limited
公开号:US04093712A1
公开(公告)日:1978-06-06
N.sup.2 -arylsulfonyl-L-argininamides and the pharmaceutically acceptable salts thereof have been found to be effective as pharmaceutical agents for the inhibition and suppression of thrombosis in mammals.
N.sup.2 -arylsulfonyl-argininamides and the pharmaceutically acceptable
申请人:Mitsubishi Chemical Industries Limited
公开号:US04101653A1
公开(公告)日:1978-07-18
N.sup.2 -arylsulfonyl-L-argininamides and the pharmaceutically acceptable salts thereof have been found to be effective as pharmaceutical agents for the inhibition and suppression of thrombosis in mammals.
N.sup.2 -alkoxynaphthylsulfonyl-L-argininamides and the pharmaceutically
申请人:Mitsubishi Chemical Industries Limited
公开号:US04073892A1
公开(公告)日:1978-02-14
N.sup.2 -alkoxynaphthylsulfonyl-L-argininamides and the pharmaceutically acceptable salts thereof have been found to be effective as pharmaceutical agents for the inhibition and suppression of thrombosis in mammals, and are prepared by reacting an N.sup.2 -alkoxynaphthylsulfonyl-L-arginyl halide with an N-substituted amino acid or an ester thereof.
N.sup.2 -alkoxynaphthalenesulfonyl-L-argininamides and the
申请人:Mitsubishi Chemical Industries Ltd.
公开号:US04055636A1
公开(公告)日:1977-10-25
N.sup.2 -alkoxynaphthalenesulfonyl-L-arginiamides and the pharmaceutically acceptable salts thereof have been found to be effective as pharmaceutical agents for the inhibition and suppression of thrombosis, and are prepared by reacting N.sup.2 -alkoxynaphthalenesulfonyl-L-arginyl halide with a secondary amine.