专利号:EP-0790982-B1 优先权日:1994-06-17 标 题 :Methods of synthesis of peptidyl argininals 发明人:WEBB THOMAS R; REINER JOHN E; TAMURA SUSAN Y; RIPKA WILLIAM C; DAGNINO RAYMOND JR; NUTT RUTH F 权利人:CORVAS INT INC 摘要:This invention provides solution-phase and solid-phase methods for the synthesis of peptidyl argininals and to novel reagents useful therein, which have formula (I), wherein R1 is selected from the group consisting of hydrogen, benzyloxycarbonyl, isonicotinyloxycarbonyl, 2-chlorobenzyloxycarbonyl, 4-methoxybenzyloxycarbonyl, t-butoxycarbonyl, t-amyloxycarbonyl, isobornyloxycarbonyl, adamantyloxycarbonyl, 2-(4-biphenyl)-2-propyloxycarbonyl, 9-fluorenylmethoxycarbonyl and methylsulfonylethoxycarbonyl; R2 is selected from the group consisting of alkyl of 1 to about 12 carbon atoms and aralkyl of about 7 to about 15 carbon atoms, either of which is optionally substituted with hydroxy or -CO-Y, wherein Y is hydroxy, alkoxy of 1 to about 12 carbon atoms, aralkoxy of about 7 to about 15 carbon atoms, O-polymeric support or NH-polymeric support; R3 is selected from the group consisting of hydrogen, Fmoc, nitro, benzyloxycarbonyl, t-butoxycarbonyl and adamantyloxycarbonyl; and R4 is selected from the group consisting of hydrogen, alkyl of 1 to about 12 carbon atoms, aryl of about 6 to about 14 carbon atoms and aralkyl of about 7 to about 15 carbon atoms; and salts thereof.
专利号:US-4940797-A 优先权日:1989-03-23 标题:Process for synthesis of FK-506 C10-C18 intermediates 发明人:JONES TODD K; MILLS SANDER G; DESMOND RICHARD 权利人:MERCK & CO INC 摘要:A process is described for the improved synthesis of the optically pure C 10 -C 18 fragment of the macrolide structure of the immunosuppressant FK-506. This compound is also useful as an intermediate for preparing FK-506 derivatives.
专利号:US-5731413-A 优先权日:1994-06-17 标 题:Method of synthesis of peptidyl aldehydes 发明人:WEBB THOMAS ROY; REINER JOHN EUGENE; TAMURA SUSAN YOSHIKO; RIPKA WILLIAM CHARLES; DAGNINO JR RAYMOND; NUTT RUTH FOELSCHE 权利人:CORVAS INT INC 摘要:This invention provides solution-phase and solid-phase methods for the synthesis of peptidyl argininals and to novel! reagents useful therein.
专利号:US-10456387-B2 优先权日:2011-11-29 标 题:Phacetoperane for treating of attention deficit hyperactivity disorder 发明人:KONOFAL ERIC; FIGADERE BRUNO 权利人:NLS PHARMA AG; NLS PHARMACEUTICS AG 摘要:The invention relates to the treatment of an attention deficit hyperactivity disorder (ADHD) with alpha-phenyl(piperidin-2-yl)methanol, or the pharmaceutically acceptable salts and esters thereof, in particular the acetate derivative, more particularly dextrophacetoperane. The invention additionally provides a method of synthesis of the (S,S) enantiomer of alpha-phenyl(piperidin-2-yl)methanol as well as a method of synthesis of dextrophacetoperane.
专利号:US-9403841-B2 优先权日:2012-01-25 标题:Phragamalin limonoids for the treatment of sexual dysfunction 发明人:WIKBERG JARL; JIRGENSONS AIGARS; LIEPINSH EDVARDS 权利人:DICOTYLEDON AB 摘要:The present invention relates to novel chemical compounds, to methods for synthesis of such compounds, and to the use of these novel compounds in the synthesis of other chemical compounds that, inter alia, may be used in the treatment of sexual dysfunction, and for eliciting enhancing effects on sexual behavior. The invention also relates to remarkable biological properties of the novel compounds in their capacity of inducing aggressive behavior.
专利号:US-11926633-B2 优先权日:2018-08-31 标 题:Synthesis methods for upadacitinib and intermediate thereof 发明人:WANG PENG; LI PIXU; WEI QIANG; CHENG WEN; WU HAO 权利人:SUZHOU PENGXU PHARMATECH CO LTD 摘要:The present disclosure relates to a JAK inhibitor upadacitinib intermediate and a preparation method therefor, and to a preparation method for a JAK inhibitor upadacitinib. The upadacitinib intermediate of the present application is as shown in Formula (II) or Formula (III),wherein, R is a protective group of nitrogen atoms, and R1 is an open-chain or cyclic amine group. Compared with the prior art, the method for the synthesis of upadacitinib of the present application, significantly reduces cost, is environmentally-friendly. And the quality of the final product is well controlled.