专利号:US-4045452-A 优先权日:1974-03-13 标题 :Steroid total synthesis process utilizing a cyanoalkyl A-ring precursor 发明人:COHEN NOAL; ROSENBERGER MICHAEL; SAUCY GABRIEL 权利人:HOFFMANN LA ROCHE 摘要:A multi-step, stereospecific total synthesis of steroids utilizing intermediates having a cyanoalkyl A-ring precursor is disclosed. The initial starting materials for this process are the relatively inexpensive and commercially available reagents γ-butyrolactone and sodium cyanide. The process is suitable for the preparation of racemic or optically active, medicinally valuable steroids, particularly 19-norsteroids. It is a feature of this process that conditions employed during the multiple step synthesis are selected so as to retain the normally labile nitrile group even during hydrogenation and hydrolysis steps. In this manner, it is possible to employ the nitrile group as an A-ring precursor without resorting to protective groups as wasl heretofore found necessary in previous steroid total synthesis processes.
专利号:US-4105676-A 优先权日:1975-12-22 标题 :Steroid total synthesis process utilizing a cyanoalkyl a-ring precursor 发明人:COHEN NOAL; ROSENBERGER MICHAEL; SAUCY GABRIEL 权利人:HOFFMANN LA ROCHE 摘要:A multi-step, stereospecific total synthesis of steroids utilizing intermediates having a cyanoalkyl A-ring precursor is disclosed. The initial starting materials for this process are the relatively inexpensive and commercially available reagents γ-butyrolactone and sodium cyanide. The process is suitable for the preparation of racemic or optically active, medicinally valuable steroids, particularly 19-norsteroids. It is a feature of this process that conditions employed during the multiple step synthesis are selected so as to retain the normally labile nitrile group even during hydrogenation and hydrolysis steps. In this manner, it is possible to employ the nitrile group as an A-ring precursor without resorting to protective groups as was heretofore found necessary in previous steroid total synthesis processes.
专利号:US-3965138-A 优先权日:1974-03-13 标 题:Steroid total synthesis process utilizing a cyanoalkyl A-ring precursor 发明人:COHEN NOAL; ROSENBERGER MICHAEL; SAUCY GABRIEL 权利人:HOFFMANN LA ROCHE 摘要:A multi-step, stereospecific total synthesis of steroids utilizing intermediates having a cyanoalkyl A-ring precursor is disclosed. The initial starting materials for this process are the relatively inexpensive and commercially available reagents γ-butyrolactone and sodium cyanide. The process is suitable for the preparation of racemic or optically active, medicinally valuable steroids, particularly 19-norsteroids. It is a feature of this process that conditions employed during the multiple step synthesis are selected so as to retain the normally labile nitrile group even during hydrogenation and hydrolysis steps. In this manner, it is possible to employ the nitrile group as an A-ring precursor without resorting to protective groups as was heretofore found necessary in previous steroid total synthesis processes.
专利号:US-3991084-A 优先权日:1970-08-26 标题 :Steroid total synthesis process utilizing a cyanoalkyl A-ring precursor 发明人:COHEN NOAL; ROSENBERGER MICHAEL; SAUCY GABRIEL 权利人:HOFFMANN LA ROCHE 摘要:A multi-step, stereospecific total synthesis of steroids utilizing intermediates having a cyanoalkyl A-ring precursor is disclosed. The initial starting materials for this process are the relatively inexpensive and commercially available reagents γ-butyrolactone and sodium cyanide. The process is suitable for the preparation of racemic or optically active, medicinally valuable steroids, particularly 19-norsteroids. It is a feature of this process that conditions employed during the multiple step synthesis are selected so as to retain the normally labile nitrile group even during hydrogenation and hydrolysis steps. In this manner, it is possible to employ the nitrile group as an A-ring precursor without resorting to protective groups as was heretofore found necessary in previous steroid total synthesis processes.
专利号:US-2004014168-A1 优先权日:1998-06-11 标题:Reagents and methods for library synthesis and screening 发明人:SCHREIBER STUART L; BLACKWELL HELEN E; PEREZ FERNANDEZ LUCY; TALLARICO JOHN A 权利人:HUGHES HOWARD MED INST 摘要:The invention provides novel solid supports for the synthesis of compound libraries. The solid supports have the physical capacity to deliver at least 50 nmol of compound and are functionalized with a silicon-containing linker. In one embodiment of the invention the solid support comprises a bead having a diameter of between approximately 400 and 600 μm functionalized with a silicon-containing linker. According to certain embodiments of the invention the bead is a polystyrene bead. According to certain embodiments of the invention the linker is a diisopropylalkyl-substituted silyl ether. The invention further provides grafted polymeric supports such as lanterns functionalized with a silicon-containing linker. n The invention provides methods for screening in which compounds are synthesized on solid supports in a quantity so that a single solid support such as a bead provides a stock solution sufficient to perform hundreds or thousands of biological or chemical assays. The methods include decoding the sequence of chemical reactions used to synthesize the compound by identifying tags incorporated into the compound during synthesis.
专利号:US-9181292-B2 优先权日:2011-01-05 标题 :Methods for preparation of glycosphingolipids and uses thereof 发明人:LIANG PI-HUI 权利人:LIANG PI-HUI 摘要:Methods for synthesis and preparation of alpha-glycosphingolipids are provided. Methods for synthesis of α-galactosyl ceramide, and pharmaceutically active analogs and variants thereof are provided. Novel alpha-glycosphingolipids are provided, wherein the compounds are immunogenic compounds which serve as ligands for NKT (natural killer T) cells.
参考标题:An Approach To Spirooxindoles Via Palladium-Catalyzed Remote C-H Activation And Dual Alkylation With Ch2Br2 作者:Changdong Shao,Zhuo Wu,Xiaoming Ji,Bo Zhou,Yanghui Zhang 摘要:A Facile And Efficient Approach For The Synthesis Of Spirooxindoles Has Been Developed Via The Coupling Of Spirocyclic C, C-Palladacycles With Ch2Br2. The Key Spirocyclic Palladacycles Are Generated Catalytically Via Intramolecular Remote C-H Activation. A Range Of Spirooxindoles Can Be Synthesized In Good To Excellent Yields From Readily Available Starting Materials.
合成参考文献
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